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AS604872 

Cat. No. M30365
AS604872  Structure
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Quality Control & Documentation
Biological Activity

AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.

Chemical Information
Molecular Weight 515.65
Formula C28H25N3O3S2
CAS Number 612532-48-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Qendresa Beqiraj-Zeqiraj, et al. Pediatr Pulmonol. Rho-kinase inhibitors protect against neonatal hyperoxia-induced airway hyperreactivity in a rat pup model: Role of prostaglandin F2α

[2] Najam A Sharif, et al. Br J Pharmacol. Prostaglandin FP receptor antagonists: discovery, pharmacological characterization and therapeutic utility

[3] Miyuki Fukuda, et al. J Pharmacol Sci. Exacerbation of intracranial aneurysm and aortic dissection in hypertensive rat treated with the prostaglandin F-receptor antagonist AS604872

[4] Rocco Cirillo, et al. Am J Obstet Gynecol. Arrest of preterm labor in rat and mouse by an oral and selective nonprostanoid antagonist of the prostaglandin F2alpha receptor (FP)

[5] André Chollet, et al. BMC Pregnancy Childbirth. Tocolytic effect of a selective FP receptor antagonist in rodent models reveals an innovative approach to the treatment of preterm labor

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Keywords: AS604872  supplier, Prostaglandin Receptor, inhibitors, activators


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