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Clopidogrel thiolactone

Cat. No. M22083
Clopidogrel thiolactone Structure
Size Price Availability Quantity
10mg USD 540  USD540 In stock
50mg USD 1080  USD1080 In stock
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Quality Control & Documentation
Biological Activity

Clopidogrel thiolactone

Chemical Information
Molecular Weight 337.82
Formula C16H16ClNO3S
CAS Number 1147350-75-1
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hong-Guang Xie, et al. J Cardiovasc Pharmacol. Overcoming Clopidogrel Resistance: Three Promising Novel Antiplatelet Drugs Developed in China

[2] Patrick M Dansette, et al. Chem Res Toxicol. Thiolactone sulfoxides as new reactive metabolites acting as bis-electrophiles: implication in clopidogrel and prasugrel bioactivation

[3] Yaoqiu Zhu, et al. Chem Res Toxicol. In vitro biotransformation studies of 2-oxo-clopidogrel: multiple thiolactone ring-opening pathways further attenuate prodrug activation

[4] Nagy A Farid, et al. J Clin Pharmacol. Metabolism and disposition of the thienopyridine antiplatelet drugs ticlopidine, clopidogrel, and prasugrel in humans

[5] Yumi Nishiya, et al. Drug Metab Dispos. Mechanism-based inhibition of human cytochrome P450 2B6 by ticlopidine, clopidogrel, and the thiolactone metabolite of prasugrel

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