- Bacterial DNA gyrase (topoisomerase II) – Fluoroquinolone antibiotic that inhibits bacterial DNA replication [2]
- Edwardsiella ictaluri – Bactericidal antibacterial agent effective against this catfish pathogen [2]

- Sarafloxacin is a potent antibacterial with minimum inhibitory concentrations (MICs) of ≤0.1 μg/mL against many important animal health pathogens (gram-negative bacteria); several gram-positive bacteria were found to be less sensitive, and fungi were not inhibited [1]
- Sarafloxacin demonstrated stability in extraction solvents (acetonitrile:water, 1:1, v/v; and pipermidic acid:KOH solution) with no degradation observed when standard was exposed to these solvents [1]
- In soil extraction studies, ACN:H₂O extractable radioactivity of ¹⁴C-sarafloxacin was less than 1% of applied radioactivity [1]
- HPLC analysis of ACN:H₂O extracts showed several components, all less than 1% of applied radioactivity; PIP:KOH extracts showed two major components: a polar component (retention time ~4-5 min) and unchanged sarafloxacin (retention time ~35 min) [1]
- The polar degradation component was acid-hydrolyzable and converted back to sarafloxacin when extracts were subjected to acid hydrolysis (2 N HCl, 60°C for 10 min) [1]
- Sarafloxacin was recovered intact from extracts of pure sand spiked with ¹⁴C-sarafloxacin, with little or no transformation observed [1]
- Sterile soils showed similar HPLC component profiles to nonsterile soils, indicating that transformation of sarafloxacin is an abiotic, soil-related phenomenon [1]

- In three field trials with channel catfish naturally infected with Edwardsiella ictaluri, sarafloxacin administered in feed for 5 days at 10 or 12.5 mg/kg of fish significantly improved survival (P < 0.05) compared to nonmedicated controls [2]
- Trial 1: Nonmedicated survival 43%, sarafloxacin-medicated (12.5 mg/kg) survival 68%; weight gain was significantly higher (3.9 g vs 2.3 g, P < 0.05) [2]
- Trial 2: Nonmedicated survival 11%, sarafloxacin-medicated (10 mg/kg) survival 48%; survival difference significant (P < 0.05) regardless of survival equation used [2]
- Trial 3: Nonmedicated survival 59%, sarafloxacin-medicated (10 mg/kg) survival 73%, Romet-medicated (100 mg/kg, twice recommended dose) survival 82%; both medicated groups had significantly higher survival and weight gain than nonmedicated controls (P < 0.05) [2]
- In trial 3, fish fed sarafloxacin-medicated feed gained 6.9 g (range 6.3-7.4 g) compared to 5.8 g for nonmedicated fish, representing approximately 8% higher final weight [2]
- In trial 1, weight gain was 40% higher in medicated fish, representing approximately 10% higher final weight [2]
- Of concern, increased mortality was observed during the last days of trials 2 and 3 in fish that had received sarafloxacin-medicated feed 11-14 days earlier [2]
- In soil biodegradation study, mineralization of ¹⁴C-sarafloxacin to ¹⁴CO₂ was low: 0.58% in loam soil (80 days), 0.49% in silt loam soil (73 days), and 0.57% in sandy loam soil (66 days) [1]
- Organic volatiles were less than 0.01% of applied radioactivity [1]

- Soil biodegradation study: Three soil types (loam, silt loam, sandy loam) with varying organic matter content (5.8%, 2.5%, 1.3% respectively). Approximately 50 g (dry weight equivalent) of soil per flask. ¹⁴C-sarafloxacin hydrochloride (specific activity 55.6 mCi/mmol or 131.8 μCi/mg) was applied at 26.52 μCi or 0.20 mg per 50 g soil (4 μg/g soil). Unlabeled glucose (~10 mg carbon per 50 g soil) was added as carbon source. Soils were incubated in the dark at 22 ± 3°C. Trapping solutions were collected at 3, 5, 7, 14, 28, 42, 56 days and at termination (sandy loam: day 66, silt loam: day 73, loam: day 80). Water was added to maintain soils at 50-70% field capacity [1]
- Field trial 1: Six 0.9 m square polyethylene net-pens (0.6 cm mesh) in earthen pond (0.9 m depth). Channel catfish fingerlings (10-13 cm, average 12 g), 150 fish per pen. Medicated feed contained 500 mg sarafloxacin/kg feed. Fish fed at 2.5% body weight (resulting in 12.5 mg sarafloxacin/kg fish) for 5 consecutive days. Nonmedicated controls fed same rate. After 5-day treatment, all fish fed nonmedicated feed at 3% body weight for 14 days. Fish counted and weighed at termination [2]
- Field trial 2: 0.40 hectare pond (1.2 m depth). Twelve net-pens (diameter 1.2 m, depth 1.2 m, 0.6 cm mesh). Channel catfish fingerlings (7-11 cm, average 6.8 g), 200 fish per pen. Medicated feed containing 500 mg sarafloxacin/kg fed at 2% body weight (10 mg/kg fish) for 5 days. Nonmedicated controls fed same rate. Treatment initiated when first E. ictaluri-related death confirmed. After 5-day treatment, all fish fed nonmedicated feed at 3% body weight for 14 days [2]
- Field trial 3: Six 0.06 hectare ponds (1.2 m depth). Three net-pens (2.4 × 1.2 × 1.2 m, 0.6 cm mesh) per pond. Channel catfish fingerlings (7-10 cm, average 6.5 g), 250 fish per pen. Treatments: sarafloxacin-medicated feed (500 mg/kg, 2% body weight = 10 mg/kg fish), Romet-medicated feed (sulfadimethoxine-ormetoprim, 100 mg/kg fish, twice recommended dose), or nonmedicated feed. Fed for 5 consecutive days. Disease transmission ensured by adding naturally infected fish (~3,000 per pond) and immersion in 10,000 E. ictaluri cells/mL for 60 seconds [2]
- Soil extraction procedure: Soils extracted with acetonitrile:water (1:1, v/v), centrifuged at 3,000-3,500 rpm for 10 min. Supernatant decanted. Soil pellets further extracted with pipermidic acid:KOH (400 mg:1 mL of 1 N KOH). First extraction with 100 mL shaking overnight, subsequent extractions with 50 mL for 2 hours. Pooled extracts analyzed by HPLC [1]
- Soil combustion: After PIP:KOH extraction, soil residues air-dried, homogenized, and triplicate aliquots oxidized to determine radioactivity bound to soil [1]
- HPLC analysis conditions: Nucleosil C18 column (150 × 4.6 mm, 5 μm particle size); flow rate 1.0 mL/min; mobile phase A: 0.1% trifluoroacetic acid (aq), mobile phase B: acetonitrile:methanol (60:40, v/v); gradient elution; detection at 280 nm; radioactivity detector with 600 μL liquid cell [1]
- Acid hydrolysis: Equal volumes of PIP:KOH extracts and 2 N HCl mixed in vials, heated at 60°C for approximately 10 minutes, then analyzed by HPLC [1]

Absorption, Distribution and Excretion
Six laying hens were orally administered (14) C-sarafloxacin for five consecutive days. Eggs were collected for 15 consecutive days after the first administration. Yolks and albumens were separated, and total radioactive residues (TRR) were determined using a combustion oxidizer and scintillation counting method. Radioactivity was detectable in both yolks and albumens on the second day after administration and peaked 24 hours after discontinuation. Subsequently, the TRR level of sarafloxacin in albumens decreased rapidly and was undetectable 2 days after the last administration; while the TRR level in yolks decreased much more slowly and was undetectable 7 days after discontinuation. High-performance liquid chromatography analysis showed that the maternal drug sarafloxacin was the main component in both egg whites and yolks. This study determined the pharmacokinetics of the fluoroquinolone antibiotic sarafloxacin in pigs and broilers. Pigs were administered a single intravenous (iv), intramuscular (im), or oral (po) dose of 5 mg/kg (pigs) and 10 mg/kg (broilers), respectively. Plasma concentration curves were analyzed using a non-compartmental pharmacokinetic model. The elimination half-lives for pigs after intravenous, intramuscular, and oral administration were 3.37 ± 0.46, 4.66 ± 1.34, and 7.20 ± 1.92 h, respectively, while those for broilers were 2.53 ± 0.82, 6.81 ± 2.04, and 3.89 ± 1.19 h, respectively. The bioavailability (F) for pigs after intramuscular and oral administration was 81.8 ± 9.8% and 42.6 ± 8.2%, respectively, while that for broilers was 72.1 ± 8.1% and 59.6 ± 13.8%, respectively. The steady-state volume of distribution (Vd(ss)) in pigs and broilers were 1.92 ± 0.27 L/kg and 3.40 ± 1.26 L/kg, respectively, and the total clearance (ClB) were 0.51 ± 0.03 L/kg/hr and 1.20 ± 0.20 L/kg/hr, respectively. In addition, the area under the curve (AUC), mean residence time (MRT), and mean absorption time (MAT) were determined. The results showed that compared with pigs, broilers absorbed sarafloxacin more quickly, distributed it more widely, and eliminated it more rapidly. Based on the determined single-dose pharmacokinetic parameters, the recommended dosing regimen is: 10 mg/kg intramuscularly every 12 hours for pigs and orally every 8 hours for broilers, which can maintain an effective plasma concentration during bacterial infection, at which the MIC90 < 0.25 μg/mL. This study investigated the absorption, metabolism, and excretion of 14C-labeled sarafloxacin in 3-month-old female New Zealand white rabbits. Animals were divided into two groups of three. One group received 10 mg/kg body weight of 14C-labeled sarafloxacin via gavage. The other three groups received the same dose intravenously. Blood samples were collected from one group at 1, 3, 6, 12, and 24 hours after oral administration, and urine and fecal samples were collected daily from the other two groups for five consecutive days. Within five days of oral administration, approximately 11% of the dose was excreted in the urine and approximately 79% in the feces. Urinary excretion after intravenous administration indicated that approximately 16% of the oral dose was absorbed systemically. Eighteen male and female Sprague-Dawley rats were randomly divided into five groups and treated with sarafloxacin: one group received a single intravenous injection of 20 mg/kg body weight; three groups received a single oral dose of 20, 75, or 275 mg/kg body weight, respectively; and the fifth group received a daily oral dose of 1000 mg/kg body weight for 14 consecutive days. Blood samples were collected from four rats in each group on day 1 of the single-dose group, before administration and at 0.5, 1, 2, 4, 6, 8, 12, and 24 hours after administration, and on days 1 and 14 of the 14-day administration group. The concentration-time area (AUC) of sarafloxacin after a single intravenous or oral administration of 20 mg/kg body weight indicated a bioavailability of approximately 12%. The AUC versus dose curve was linear below 275 mg/kg body weight, but deviated from linearity at 1000 mg/kg body weight. For more complete data on absorption, distribution, and excretion of sarafloxacin (8 items in total), please visit the HSDB record page.

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Metabolism/Metabolites
This study investigated the pharmacokinetics and metabolism of sarafloxacin in two groups of six volunteers (single oral doses of 100 mg or 200 mg, respectively) and two groups of five volunteers (single oral doses of 400 mg or 800 mg, respectively). …The metabolism of sarafloxacin appears to involve primarily the oxidative degradation of the piperazine substituent, initially producing 3'-oxosarafloxacin. Subsequent oxidation produces an ethylenediamine-substituted quinolone, which is further oxidized to an aminoquinolone. Plasma concentrations of the ethylenediamine-substituted quinolone were similar to those of the parent drug, but its mean AUC was consistently only about 6% of that of sarafloxacin. Concentrations of the aminoquinolone in plasma and urine were significantly lower than those of the ethylenediamine-substituted quinolone. 3'-oxosarafloxacin was not detected in plasma due to weak fluorescence. In urine, the major drug-related peak is sarafloxacin, accounting for 75-80% of all urinary metabolites. Following sarafloxacin administration, the major urinary metabolite was preliminarily identified as 3'-oxosafloxacin, with concentrations typically one-third to one-quarter that of sarafloxacin. Total urinary recovery of the parent drug and its metabolites was low and dose-dependent, decreasing from 24% to 10% as the dose increased from 100 mg to 800 mg. This decrease was similar to the decrease in dose-normalized AUC. Aminoquinolones, ethylenediamine-substituted quinolones, and their conjugates accounted for <7% of urinary excretion. … (Breed, sex, and quantity not specified) Dogs were given an oral or intravenous dose of 10 mg/kg body weight of 14C-sarafloxacin. Approximately 79% of the 10 mg/kg body weight dose of 14C-sarafloxacin was excreted in urine and feces as unmetabolized parent drug. In bile, the proportions of unmetabolized parent drug and its glucuronide are approximately equal. To investigate the microbial biotransformation of veterinary fluoroquinolones, Mucor ramannianus was cultured for 18 days in a sucrose/peptone broth containing sarafloxacin. The culture was extracted with ethyl acetate, and the extract was analyzed by liquid chromatography. Two metabolites (26% and 15% of A280, respectively) were identified by mass spectrometry and 1H NMR spectroscopy: N-acetylsarafloxacin and desethylene-N-acetylsarafloxacin. The biosynthesis of desethylene-N-acetylsarafloxacin has not been previously reported. Biological half-life: Twenty-two healthy male volunteers aged 20 to 39 years were administered single oral doses of 100, 200, 400, or 800 mg of sarafloxacin. …At doses of 100, 200, 400, and 800 mg, the mean terminal half-lives were 9, 9, 10, and 11 hours, respectively. This study determined the pharmacokinetics of the fluoroquinolone antibiotic sarafloxacin in pigs and broilers, administered intravenously (iv), intramuscularly (im), or orally (po), at single doses of 5 mg/kg (pigs) and 10 mg/kg (broilers), respectively. …After intravenous, intramuscular, and oral administration, the elimination half-lives in pigs were 3.37 ± 0.46, 4.66 ± 1.34, and 7.20 ± 1.92 hours, respectively, while the elimination half-lives in broilers were 2.53 ± 0.82, 6.81 ± 2.04, and 3.89 ± 1.19 hours, respectively. In this study, the pharmacokinetics of sarafloxacin were investigated in eels (Anguilla anguilla) at a dose of 15 mg/kg body weight via gavage at a water temperature of 24℃. The distribution rate constant (α) was 0.085 hr⁻¹ (r=0.972), and the half-life (t₁₀α) was 8.15 hr. The elimination rate constant (β) was 0.023 hr⁻¹ (r=0.909), and the half-life (t₁₀β) was 30.13 hr.

Toxicity Summary
Identification and Uses: Sarafloxacin is a fluoroquinolone antibacterial drug. In veterinary medicine, it is used to treat and control bacterial infections in poultry. Sarafloxacin is also used in aquaculture to treat furunculosis, vibriosis, and intestinal red mouth disease in salmonids. Human Exposure and Toxicity: The safety of a single oral dose of sarafloxacin was studied in a cohort of healthy male volunteers. Six subjects received 100 mg of sarafloxacin, six received 200 mg, five received 400 mg, and five received 800 mg. The most common adverse reactions were dizziness and fatigue. Subjects receiving the lowest dose reported mood instability, somnolence, and hiccups. A study also examined the safety of continuous oral administration of sarafloxacin for 7 days in six healthy male volunteers, who received doses of 100 mg every 12 hours, 200 mg every 12 hours, or 100 mg every 6 hours. The most common adverse reactions were fatigue and dizziness. The most common adverse reactions in the placebo group were fatigue and somnolence. Animal Studies: In a dietary palatability study, sarafloxacin was administered as a feed additive to four groups of rats (n=5 per group, 5 males and 5 females, 4-5 weeks old) for two weeks. No significant signs of toxicity or death were observed in animals fed diets containing up to 10,000 mg/kg sarafloxacin. Treatment-related side effects, including alopecia, emaciation, dehydration, decreased feed intake, and weight gain, were observed in rats fed diets containing 50,000 mg/kg sarafloxacin. In a 15-day trial, sarafloxacin was administered as a feed additive to four groups of mice (n=5 per group, 5 males and 5 females, 4-5 weeks old). Mice fed diets containing up to 10,000 mg/kg sarafloxacin showed no significant toxicity or death. In mice fed diets containing 25,000 and 50,000 mg/kg sarafloxacin, only treatment-related effects of reduced feed intake and weight gain were observed. In addition, sarafloxacin was used as a feed additive in 60 mice (60 males and 60 females, at doses of 150, 750, and 3000 mg/kg body weight/day, respectively). Ten additional mice (10 males and 10 females) from each group were hematologically evaluated and sacrificed at 52 weeks. The carcinogenicity study was terminated at 78 weeks due to excessively high mortality. Increased mortality was observed in both male and female mice in the medium and high dose groups. Nephrotoxicity was observed in females in the medium and high dose groups. Gallstones and urinary tract stones were observed in males in the high dose group. Cecal dilatation was observed in both males and females in all dose groups, and cecal volvulus was also observed in males and females in the medium and high dose groups. No evidence of carcinogenicity was found. A three-generation reproductive toxicity study in rats, with each generation containing 30 males and 30 females, was also conducted. Rat were administered sarafloxacin daily by gavage at doses of 75, 275, or 1000 mg/kg body weight, starting at least 70 days prior to breeding. Autopsy of F0 generation rats revealed red gastrointestinal contents and/or red lesions in the stomach. In first-generation female parents, both absolute and relative liver weight were significantly reduced in the medium- and high-dose groups. Second-generation male and female parents, as well as third-generation male parents, also showed significant reductions in relative liver weight in the medium- and high-dose groups. Third-generation female parents also showed a reduction in relative liver weight in the high-dose group. A developmental toxicity study was conducted in 18 artificially inseminated white rabbits across three groups, which were administered sarafloxacin daily by gavage at doses of 15, 35, or 75 mg/kg body weight/day from days 6 to 18 of gestation. Fourteen female rabbits aborted between days 21 and 29 of gestation. External examination revealed malformations in 6 fetuses from one litter in the high-dose group, reported as wrist and/or tarsal flexion. Visceral examination revealed malformations in 5 fetuses from one litter in the high-dose group, reported as hydrocephalus. Skeletal malformations were observed in 6 fetuses from one litter in the high-dose group, reported as chondroskeletal abnormalities. Malformations were observed in 3 fetuses from two litters in the medium-dose group. The only parameters unaffected by treatment were the mean number of corpora lutea, number of implantation sites, number of live fetuses per litter, and mean post-implantation loss rate at scheduled fetal retrieval. A dose-related decrease in mean fetal weight was observed at doses of 35 and 75 mg/kg body weight/day. Teratogenicity is considered secondary to maternal toxicity and not directly attributable to treatment.

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Non-human toxicity values
Oral LD50 in rats >8,000 mg/kg body weight
Oral LD50 in mice >8,000 mg/kg body weight

[1]. Aerobic biodegradation of (14C)-sarafloxacin hydrochloride in soil. Environmental Toxicology and Chemistry, 1997. 16(3): p. 462-471.

[2]. Effects of sarafloxacin hydrochloride on human enteric bacteria under simulated human gut conditions. Vet Q, 1995 Mar;17(1):1-5.

[3]. Field efficacy trials of the antibacterial sarafloxacin-hydrochloride (A-56620) for treatment of Edwardsiella ictaluri infections in channel catfish. Journal of aquatic animal health, 1992. 4(4): p. 244-251.

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid belongs to the quinoline class of compounds. Sarafloxacin is a quinolone antibiotic, and its manufacturer, Abbott Laboratories, ceased production before obtaining marketing authorization in the United States or Canada.
Therapeutic Uses
Veterinary Drug: Sarafloxacin is used to treat and control bacterial infections in poultry caused by Escherichia coli and Sarcinapterin. Veterinary Drug: The antibiotic sarafloxacin can be used to treat chickens infected with Escherichia coli serotype O78. Three trials have been conducted to study the efficacy of this drug in experimentally infected chickens with E. coli. Poultry were monitored for 10 days after infection, recording mean daily gain (ADG) and feed conversion ratio (FCR), and post-mortem pathology was evaluated. In the first experiment, adding sarafloxacin (20 mg/L, equivalent to 5 mg/kg live weight/day) to the drinking water for three consecutive days post-infection reduced the mortality rate from 75% to 27%, but the daily gain (ADG) in the treated group was still lower than that in the uninfected control group. In the second experiment, adding the same dose of sarafloxacin to the drinking water, but only for 2 hours, also significantly reduced mortality, and ADG and FCR were significantly improved. In the third experiment, the dose-dependency of the drug was tested. Each group of poultry was given 5 mg/kg/day and 10 mg/kg/day of sarafloxacin, respectively, starting 2 hours post-infection. Rapid administration completely stopped mortality, while daily gain and feed conversion ratio were similar to the uninfected control group.
Drug (Veterinary): Approved antibiotic for aquaculture: Sarafloxacin – indicated for the treatment of furunculosis, vibriosis, and intestinal red mouth disease in salmonids. /Excerpt from table/

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- Sarafloxacin hydrochloride is a fluoroquinolone antibiotic (molecular formula: C₃₈H₁F₁N₁O₃•HCl; molecular weight: 421.84; CAS registry number: 91296-87-6) registered for use against poultry diseases and tested for treatment of Edwardsiella ictaluri infections in channel catfish [1][2]
- The compound is a potent antibacterial with MICs ≤0.1 μg/mL against many gram-negative animal health pathogens [1]
- Sarafloxacin is a quinoline-3-carboxylic acid derivative: 1-(p-fluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-7-(piperazinyl)-quinoline-3-carboxylic acid [1]
- In soil, sarafloxacin strongly binds to organic matter; extractability decreased with increasing organic matter content: 25% in loam (5.8% OM), 73% in silt loam (2.5% OM), 81% in sandy loam (1.3% OM) using PIP:KOH extraction [1]
- The polar degradation component formed in soil is acid-hydrolyzable and converts back to sarafloxacin, suggesting reversible binding or complex formation [1]
- Formation of the polar component appears to be surface-catalyzed (clay, organic matter, or metals), not biologically mediated [1]
- In field trials, Romet (sulfadimethoxine-ormetoprim) at twice recommended dose (100 mg/kg) showed numerically higher survival (82%) compared to sarafloxacin (73%), but this difference was not significant in all survival calculations [2]
- Antibiotic resistance in E. ictaluri is an emerging concern: in 1990, 12 isolates resistant to oxytetracycline, 43 resistant to Romet, and 60 resistant to both were identified [2]

C20H17F2N3O3

385.37

385.124

C, 62.33; H, 4.45; F, 9.86; N, 10.90; O, 12.45

98105-99-8

Sarafloxacin hydrochloride;91296-87-6;Sarafloxacin-d8 hydrochloride trihydrate

56208

Typically exists as solid at room temperature

1.436 g/cm3

621.4ºC at 760 mmHg

112-114 °C

329.6ºC

1.633

2.77

2

8

3

28

645

0

O=C(C1=CN(C2=CC=C(F)C=C2)C3=C(C=C(F)C(N4CCNCC4)=C3)C1=O)O

XBHBWNFJWIASRO-UHFFFAOYSA-N

InChI=1S/C20H17F2N3O3/c21-12-1-3-13(4-2-12)25-11-15(20(27)28)19(26)14-9-16(22)18(10-17(14)25)24-7-5-23-6-8-24/h1-4,9-11,23H,5-8H2,(H,27,28)

6-fluoro-1-(4-fluorophenyl)-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid

A 56620; A-56620; Sarafloxacin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)