Absorption, Distribution and Excretion
Based on urine and bile data, oral absorption is high (>90%), with most of the bile component being reabsorbed and excreted in the urine. The bile component increases disproportionately with increasing dose from 15 mg/kg body weight to 600 mg/kg body weight. The radiolabeled drug is rapidly absorbed, with peak plasma concentrations reached within 0.25 to 1 hour at single doses of 600 mg/kg body weight and below. Quinocyclocarboxylic acid is widely distributed in the body, with the highest concentrations in the blood, plasma, and kidneys. Tissue concentrations are typically higher in women than in men (<2 times). The labeled drug is rapidly excreted, primarily via urine (50-90% within 24 hours). The initial plasma half-life is approximately 3-4 hours. Repeated administration of a 600 mg/kg body weight dose and a single 1200 mg/kg body weight dose slow the clearance of the drug from the blood, resulting in a disproportionate increase in the area under the concentration-time curve (AUC). Regardless of the dose level, and regardless of whether labeled or unlabeled quinclorac was administered 7 or 14 days prior to the administration of radiolabeled quinclorac, the excretion patterns and tissue distribution of radioactivity were similar. This study extensively investigated the metabolism of oral quinclorac ((2,3,4-(14)C)3,7-dichloro-8-quinolinecarboxylic acid) in male and female CD rats. Following a single oral dose of 15 or 600 mg/kg of (14)C quinclorac, and after 14 consecutive days of administration of unlabeled quinclorac at a dose of 15 mg/kg/day, followed by an oral dose of 15 mg/kg of quinclorac, the compound was rapidly absorbed and excreted in the urine. Five days after administration, 91% to 98% of the administered dose was excreted in the urine, with only 1% to 4% excreted in the feces. No radioactivity was detected in exhaled breath. Animals receiving a 600 mg/kg dose showed significant bile excretion (11.5% to 14.5% of the administered dose). However, most of the radioactive material was reabsorbed by the intestine and excreted in the urine. A large portion of the radioactive material in the bile was associated with a glucuronide conjugate of quinclorac. This conjugate was apparently hydrolyzed and reabsorbed in the intestine. Almost all the radioactive material in the urine was unmetabolized quinclorac. Five days after administration, the level of residual radioactivity in tissues was dose-dependent. These studies, along with others (whole-body autoradiography and time-course studies), suggest that quinclorac may accumulate in the adrenal glands, bone marrow, thyroid gland, squamous epithelium outside the gastric fundus, and ovaries. In a 7-day time-course study (oral dose of 15 mg/kg/day, or dietary dose of approximately 1000 mg/kg/day), the highest residual level of 14C was detected 30 minutes after the last administration; thereafter, the residual level decreased over time. In animals receiving a single oral dose of 15, 100, or 600 mg/kg or 15 mg/kg/day for 7 consecutive days, mean 14C residues were also detected in plasma at 30 minutes. Rapid elimination half-lives of 3 to 4 hours were observed in the low-dose groups, while the half-life in the 600 mg/kg dose group was approximately 13 hours, exhibiting biphasic elimination. In animals receiving higher doses (1200 mg/kg or 600 mg/kg/day for 7 consecutive days), peak plasma radioactivity levels were observed 7 to 48 hours post-administration; saturation kinetics were also observed at these higher doses. Metabolites/Metabolites…The presence of metabolites was extracted and analyzed using techniques including thin-layer chromatography and mass spectrometry. The absorbed quinclorac is metabolized to a limited extent, with approximately 80% of the excreted radiolabeled compound remaining unchanged. The major biotransformation product is the quinclorac-glucuronide conjugate, accounting for approximately 5% of the administered dose. Metabolic patterns were similar across sexes, dose levels, and repeated dosing. Some metabolites were not identified, and the levels of each metabolite were less than 5% of the administered dose. Quinolone's metabolism is very limited, therefore no metabolic pathway is required. Biological Half-Life In a 7-day time-course study (administered orally at 15 mg/kg/day; or via diet at approximately 1000 mg/kg/day), the maximum ¹⁴C residual level was detected 30 minutes after the last dose; thereafter, the residual level decreased over time. … Its elimination process is biphasic, with a rapid elimination half-life of 3 to 4 hours at low doses, compared to approximately 13 hours at a dose of 600 mg/kg. …

[1]. Cavalheiro de Menezes C, et al. The effects of diphenyl diselenide on oxidative stress biomarkers in Cyprinus carpio exposed to herbicide quinclorac (Facet®). Ecotoxicol Environ Saf. 2012;81:91-97.

Quinclorac is a quinoline monocarboxylic acid, namely quinoline-8-carboxylic acid, in which the hydrogen atoms at positions 3 and 7 are replaced by chlorine atoms. It (especially its dimethylamine salt, dimethylammonium quinoxalate) is used as a post-emergence weed control agent for rice, lawns, and grasslands (a relatively long-lasting herbicide). It is not approved for use in the European Union. It has multiple uses as a herbicide, agrochemical, and synthetic growth regulator. It is a quinoline monocarboxylic acid, an organochlorine compound, and a monocarboxylic acid. It is the conjugate acid of Quinclorac (1-). Quinclorac is a selective herbicide primarily used for weed control in rice paddies, but it is also used in other crops and is found in some household lawn herbicides.

C10H5CL2NO2

242.06

240.969

84087-01-4

91739

White/yellow solid
Colorless crystalline solid

1.6±0.1 g/cm3

405.4±40.0 °C at 760 mmHg

274ºC

199.0±27.3 °C

0.0±1.0 mmHg at 25°C

1.695

2.11

1

3

1

15

262

0

O=C(C1C2C(=CC(=CN=2)Cl)C=CC=1Cl)O

FFSSWMQPCJRCRV-UHFFFAOYSA-N

InChI=1S/C10H5Cl2NO2/c11-6-3-5-1-2-7(12)8(10(14)15)9(5)13-4-6/h1-4H,(H,14,15)

3,7-dichloroquinoline-8-carboxylic acid

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)

DMSO: 125 mg/mL (516.40 mM)

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.)