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Nevanimibe hydrochloride

Cat. No. M14293
Nevanimibe hydrochloride Structure
Synonym:

PD-132301 hydrochloride; ATR101 hydrochloride

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Quality Control & Documentation
Biological Activity

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.

Chemical Information
Molecular Weight 458.08
CAS Number 133825-81-7
Solubility (25°C) DMSO 41.67 mg/mL
Storage 2-8°C, dry, sealed
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] Diala El-Maouche, et al. J Clin Endocrinol Metab. A Phase 2, Multicenter Study of Nevanimibe for the Treatment of Congenital Adrenal Hyperplasia

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Abmole Inhibitor Catalog




Keywords: Nevanimibe hydrochloride, PD-132301 hydrochloride; ATR101 hydrochloride supplier, inhibitors, activators


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