PF-3882845

PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM[1].

Product Specifications

CAS Number

[1023650-66-9]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Mineralocorticoid Receptor; Progesterone Receptor

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pf-3882845.html

Purity

99.90

Solubility

DMSO : 10 mg/mL (ultrasonic; warming)

Smiles

N#CC1=CC=C(N2N=C(C(C=CC(C(O)=O)=C3)=C3CC4)[C@H]4[C@@H]2C5CCCC5)C=C1Cl

Molecular Formula

C24H22ClN3O2

Molecular Weight

419.90

Precautions

H315, H319, H335

References & Citations

[1]Meyers MJ, et al. Discovery of (3S,3aR) -2- (3-chloro-4-cyanophenyl) -3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy. J Med Chem. 2010 Aug 26;53 (16) :5979-6002.