At a minimum inhibitory concentration (MIC) of 0.05 to 1 μg/mL, cefclodine can inhibit the following pathogens: Staphylococcus aureus, penicillin-sensitive and penicillin-resistant strains, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae, Clostridium septicarum, etc. [1].

In rabbits and monkeys, cefclodine (50–500 mg/kg; intramuscular injection) shows dose-related nephrotoxicity [2].

Animal/Disease Models: Rabbits and monkeys [2]
Doses: 50, 100, 200 and 500 mg/kg
Route of Administration: intramuscularinjection
Experimental Results: 200 and 500 mg/kg caused significant changes in renal function and proximal tubule necrosis. Renal impairment does not appear to occur at doses of 50 and 100 mg/kg.

Absorption, Distribution and Excretion
Renal.
.../CEPHALORIDINE/ POORLY ABSORBED FROM GI TRACT. PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED; 10 TO 20% OF PLASMA CEPHALORIDINE IS BOUND TO PROTEIN.
IM INJECTIONS OF 0.5 & 1 G YIELD PEAK PLASMA CONCN OF 15 & 30 UG/ML, RESPECTIVELY. APPROX 75% OF GIVEN DOSE IS EXCRETED IN URINE, MAINLY BY GLOMERULAR FILTRATION. CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH...
PLACENTAL DRUG TRANSFER- CEPHALORIDINE: TIME TO APPEAR IN FETUS 30 MIN; TIME TO FETAL/MATERNAL CONCN EQUIL 5 HR. /FROM TABLE/
.../CEPHALORIDINE/ READILY PENETRATE NORMAL EYE FOLLOWING SYSTEMIC OR SUBCONJUNCTIVAL ADMIN...
...CEPHALORIDINE...SHOWN...TO PENETRATE INTO BONE TO VERY LIMITED EXTENT AFTER SC OR ORAL DOSES TO RATS. RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER DOSING.

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Biological Half-Life
.../CEPHALORIDINE/ PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED... WHILE ITS T/2 (60 TO 90 MIN)...ONLY SMALL AMT ARE DETECTABLE AFTER 8 HR.
/IN RATS/ RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER /ORAL OR SC/ DOSING. DESPITE DIFFERENCES IN CONCN, T/2 IN BONE & SERUM WERE SIMILAR.

Interactions
NON-IONIC, ANIONIC, & ZWITTERIONIC SURFACTANTS INDUCED RAPIDLY REVERSIBLE HYPER-ABSORPTIVE STATE IN THOMAS CANINE FUNDIC POUCH FOR CEPHALORIDINE...BLOOD LEVELS...MANY TIMES GREATER THAN VALUES IN CONTROLS.
CEPHALORIDINE SEEMS TO HAVE GREATEST POTENTIAL FOR NEPHROTOXICITY.../IT SHOULD NOT/ BE USED WITH GENTAMICIN /OR OTHER AMINOGLYCOSIDES, AMIKACIN, NEOMYCIN, PAROMOMYCIN & TOBRAMYCIN/ UNLESS LIFE-THREATENING CONDITION EXISTS /MAY INCR NEPHROTOXICITY/.
CEPHALORIDINE NEPHROTOXICITY IS ENHANCED BY CONCURRENT FUROSEMIDE ADMIN. SUCH THERAPY SHOULD BE AVOIDED IN PATIENTS WHO HAVE EVEN MILD PREEXISTING RENAL DISEASE.
...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION OF...WEAK ACIDS COULD RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/
Groups of ten male rats were treated with a high challenge dose of cephaloridine (3750 mg/kg), with methylprednisolone (100 mg/kg) or with cephaloridine and methylprednisolone by single sc injection. A control group received the injection vehicles only. Urine was collected from all animals daily over 18-hr collection periods, up to 96 hr after treatment. Blood was collected at 24, 48, 72 and 96 hr after treatment. At necropsy, kidneys were weighed, processed and examined histopathologically. Results show that methylprednisolone significantly ameliorated the nephrotoxicity of the challenge dose of cephaloridine. Cephaloridine-only treated rats had severe toxic nephrosis characterized by acute tubular necrosis, and elevated blood urea and creatinine. by contrast, the majority of cephaloridine plus methylprednisolone treated rats had only a slight or moderate toxic nephrosis, and had lower blood urea and creatinine levels compared with rats treated with cephaloridine only, indicating preservation of kidney function. Interestingly, rats treated with cephaloridine and methylprednisolone had higher urinary enzymes ... as well as protein and glucose, compared with rats treated with cephaloridine only. this is taken to indicate that rats treated with cephaloridine only had such marked kidney damage and necrosis that the population of cells able to produce these marker enzymes was significantly and rapidly depleted, but the protection afforded by methylprednisolone allowed cephaloridine plus methylprednisolone treated rats to sustain urinary enzyme output. Effects on urinary glucose and other parameters ... demonstrate interactions between glucocorticoid pharmacology and cephaloridine nephrotoxicity.

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Non-Human Toxicity Values
LD50 MOUSE ORAL GREATER THAN 15 G/KG
LD50 MONKEY INTRAMUSCULAR GREATER THAN 0.2 G/KG

[1]. P. W. Muggleton, et al. Laboratory Evaluation of a New Antibiotic-Cephaloridine (Ceporin). Br Med J. 1964 Nov 14;2(5419):1234-7.
[2]. Perkins RL, et al. Cephaloridine and cephalothin: comparative studies of potential nephrotoxicity. J Lab Clin Med. 1968 Jan;71(1):75-84.

Cefaloridine is a cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C. It has a role as an antibacterial drug. It is a cephalosporin, a semisynthetic derivative and a beta-lactam antibiotic allergen.
Cephaloridine or cefaloridine is a first generation semisynthetic cephalosporin. It is derived from cephalosporin C and is a zwitterion at physiological pH.
Cephaloridine is a semisynthetic, broad-spectrum, first-generation cephalosporin with antibacterial activity. Cephaloridine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
A cephalosporin antibiotic.

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Mechanism of Action
CEPHALOTHIN & ITS CONGENERS INHIBIT BACTERIAL CELL-WALL SYNTHESIS IN MANNER SIMILAR TO THAT OF PENICILLIN. /CEPHALOSPORINS/
Cephaloglycin and cephaloridine are acutely toxic to the proximal renal tubule, in part because of their cellular uptake by a contraluminal anionic secretory carrier and in part through their intracellular attack on the mitochondrial transport and oxidation of tricarboxylic acid (TCA) cycle anionic substrates. Preliminary studies with cephaloglycin have provided evidence of a role of fatty acid (FA) metabolism in its nephrotoxicity, and work with cephaloridine has shown it to be a potent inhibitor of renal tubular cell and mitochondrial carnitine (Carn) transport.

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Therapeutic Uses
Cephalosporins
GENERAL RANGE OF ACTIVITY & ANTIBACTERIAL SPECTRUM OF CEPHALORIDINE CLOSELY APPROX THAT OF CEPHALOTHIN, ALTHOUGH SOME STRAINS OF E COLI MAY BE SOMEWHAT MORE SENSITIVE TO FORMER. IT ALSO APPEARS TO BE MORE ACTIVE THAN CEPHALOTHIN AGAINST CL PERFRINGENS (WELCHII). MYCOBACTERIUM FORTUITUM IS SENSITIVE TO CEPHALORIDINE...
CEPHALORIDINE...GIVEN PARENTERALLY & SUBCONJUNCTIVALLY TO TREAT INTRAOCULAR INFECTIONS & MAY BE ADMIN TOPICALLY & SUBCONJUNCTIVALLY TO TREAT CORNEAL ULCERS.
CEPHALORIDINE IS EFFECTIVE IN THERAPY OF BRONCHITIS DUE TO H INFLUENZAE, BUT OTHER AGENTS OFTEN PRODUCE BETTER RESULTS, THIS DRUG HAS ALSO BEEN FOUND USEFUL WHEN EMPLOYED AS AEROSOL IN PATIENT WITH PURULENT BRONCHITIS.
For more Therapeutic Uses (Complete) data for CEPHALORIDINE (10 total), please visit the HSDB record page.

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Drug Warnings
CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH; SINGLE DOSE OF 1 G IM YIELDS DETECTABLE CONCN FOR AS LONG AS 4 DAYS. ...CEPHALORIDINE SHOULD NOT BE GIVEN TO SUCH PATIENTS, SINCE IT IS NEPHROTOXIC.
WHILE CEPHALORIDINE PRODUCES LESS IRRITATION /THAN CEPHALOTHIN/, ITS NEPHROTOXICITY OUTWEIGHS THIS ADVANTAGE.
IN 48-HR HUMAN INFANTS...CEPHALORIDINE...HAVE VERY LONG PLASMA T/2, & TOXIC CONCN ARE REACHED WHEN DOSES ARE LOWERED CONSIDERABLY.
CEPHALORIDINE IS INJECTED EITHER IM OR IV. ... SINCE OTHER, LESS TOXIC CEPHALOSPORINS ARE AVAIL, THERE IS NO REASON TO RECOMMEND THIS PREPN.
For more Drug Warnings (Complete) data for CEPHALORIDINE (7 total), please visit the HSDB record page.

C19H17N3O4S2

415.482

415.066

50-59-9

Cephaloridine hydrate;102039-86-1

5773

CRYSTALS
WHITE TO OFF-WHITE, CRYSTALLINE POWDER

184°C

0.011

1

6

5

28

687

2

O=C([O-])C=1N2C([C@@H](NC(CC3=CC=CS3)=O)[C@H]2SCC1C[N+]4=CC=CC=C4)=O

CZTQZXZIADLWOZ-CRAIPNDOSA-N

InChI=1S/C19H17N3O4S2/c23-14(9-13-5-4-8-27-13)20-15-17(24)22-16(19(25)26)12(11-28-18(15)22)10-21-6-2-1-3-7-21/h1-8,15,18H,9-11H2,(H-,20,23,25,26)/t15-,18-/m1/s1

(6R,7R)-8-oxo-3-(pyridin-1-ium-1-ylmethyl)-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

Cefaloridine; Cephaloridine; Sch 11527

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.)