| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
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| ln Vivo |
Good sex dogs with osteoarthritis can benefit from a 14-day regimen of oral tube feeding (cinchophen; 25–44 mg/kg; twice daily) plus prednisolone (0.125–0.220 mg/kg; twice daily). This combination is both efficacious and well-tolerated. With clinical efficacy comparable to phenylbutazone, the combination markedly improved lameness, weight-bearing, joint mobility, and stiffness scores [2]. Testing was done on the kinetics and effectiveness of a combined formulation of prednisolone (PLT) and cincophenol. A dose of 12.5 mg/kg of cinchophen was given intravenously. Its volume of distribution (Vd area) was 0.13 L/kg, its clearance (Cl) was 0.15 L/h, and its half-life (t1/2β) was 7.92 hours. In dogs, the AUC0-∞ for blood drug concentration-time curve is 1187.0 μ/ml.h[2]. A single dose of 12.5 mg/kg of cinchophene administered orally produced a mean maximum plasma concentration (Cmax) of 77.75 μg/ml and a time to Cmax (tmax) of 2.76 hours. Oral dosing results in a plasma concentration-time curve (AUC0-∞) that is nearly twice as large as intravenous administration, meaning that oral bioavailability (F) is 87.21% [2].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
2% 2-O-OXYPHENYLQUINOLINE-4-CARBOXYLIC ACID WAS EXCRETED IN URINE FROM HUMANS AFTER DOSAGE WITH CINCHOPHEN. /FROM TABLE/ YIELDS 8-HYDROXY-2-PHENYLQUINOLINE-4-CARBOXYLIC ACID & 2-(P-HYDROXYPHENYL)QUINOLINE-4-CARBOXYLIC ACID IN DOG: HARTIALA, K, TERHO, T & HAKKINEN, I; BIOCHEM PHARMAC, 16, 843 (1967). /FROM TABLE/ Biological Half-Life IN BLOOD OF HUMANS HALF LIFE AFTER DOSAGE OF CINCHOPHEN WAS 4-4.5 HR. |
| Toxicity/Toxicokinetics |
Interactions
IN DOGS, CINCHOPHEN HAD NO EFFECT ON IOPANOIC ACID EXCRETIO BUT INCR BOTH BILIARY & URINARY EXCRETION OF IOPHENOXIC ACID. |
| References |
[1]. R.G. Snyder, M.D, et al. The use of cinchophen in the treatment of chronic arthritis. THE AMERICAN ASSOCIATION FOR THE STUDY AND CONTROL OF RHEUMATIC DISEASE
[2]. Q. A. McKellar, et al. Pharmacokinetics and clinical efficacy of a cinchophen and prednisolone combination in the dog. Jsap. Volume32, Issue2. February 1991 |
| Additional Infomation |
2-phenyl-4-quinolinecarboxylic acid is a member of quinolines.
Therapeutic Uses Anti-Inflammatory Agents, Non-Steroidal /IT WAS USED AS/ ANALGESIC IN ACUTE GOUT, ACTING MORE PROMPTLY THAN COLCHICUM & WITHOUT UNDESIRABLE SIDE EFFECTS. ... DOSE: ORAL, 0.5 G. ONCE USED AS URICOSURIC, ANALGESIC & ANTI-INFLAMMATORY AGENT Drug Warnings THE OCCURRENCE OF JAUNDICE WITH CINCHOPHEN & ITS VARIOUS DERIV WAS OBSERVED WITH SUCH FREQUENCY & HERALDED SUCH SEVERE DEGENERATIVE & NECROTIZING CHANGES IN LIVER THAT THESE DRUGS HAVE BEEN LARGELE ABANDONED. QUINIDINE, ADMIN PARENTERALLY SHORTLY AFTER OR SIMULTANEOUSLY WITH TUBOCURARINE, MAY ENHANCE OR CAUSE RECURRENT NEUROMUSCULAR EFFECTS OF TUBOCURARINE... ALTHOUGH NO DRUG INTERACTION HAS BEEN DOCUMENTED, OTHER CINCHONA ALKALOIDS (EG CINCHOPHEN & QUININE) MAY ALSO INTERACT WITH TUBOCURARINE. CLINICAL & EXPTL STUDIES SHOW THAT ANTIARRHYTHMIC & CARDIODEPRESSANT EFFECTS OF QUINIDINE MAY BE ENHANCED BY ADMIN OF RESERPINE. ... CINCHOPHEN & QUININE ARE AGENTS RELATED TO QUINIDINE. THE OTHER CINCHONA ALKALOIDS, CINCHOPHEN & QUININE, APPARENTLY EXERT DIRECT HYPOPROTHROMBINEMIC EFFECT BY DEPRESSING THE HEPATIC ENZYME SYSTEM THAT SYNTHESIZES VITAMIN K-DEPENDENT FACTORS...& COULD INTERACT WITH WARFARIN ALSO. |
| Molecular Formula |
C16H11NO2
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|---|---|
| Molecular Weight |
249.27
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| Exact Mass |
249.078
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| CAS # |
132-60-5
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| PubChem CID |
8593
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| Appearance |
NEEDLES FROM METHANOL OR DILUTED ALCOHOL
WHITE OR YELLOWISH CRYSTALS OR POWDER SMALL, WHITE, NEEDLE-LIKE CRYSTALS |
| Density |
1.3±0.1 g/cm3
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| Boiling Point |
456.9±33.0 °C at 760 mmHg
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| Melting Point |
213-216ºC
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| Flash Point |
230.1±25.4 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.682
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| LogP |
3.99
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
325
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C(C1=C([H])C(C2C([H])=C([H])C([H])=C([H])C=2[H])=NC2=C([H])C([H])=C([H])C([H])=C21)=O
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| InChi Key |
YTRMTPPVNRALON-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11NO2/c18-16(19)13-10-15(11-6-2-1-3-7-11)17-14-9-5-4-8-12(13)14/h1-10H,(H,18,19)
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| Chemical Name |
2-phenylquinoline-4-carboxylic acid
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| Synonyms |
Agotan; Mylofanol; Cinchopen
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~334.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0117 mL | 20.0586 mL | 40.1171 mL | |
| 5 mM | 0.8023 mL | 4.0117 mL | 8.0234 mL | |
| 10 mM | 0.4012 mL | 2.0059 mL | 4.0117 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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