1. Metabolic Enzyme/Protease
    Others
  2. Mineralocorticoid Receptor
    Progesterone Receptor
  3. PF-3882845

PF-3882845 

Cat. No.: HY-12738
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-3882845 Chemical Structure

PF-3882845 Chemical Structure

CAS No. : 1023650-66-9

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Description

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].

IC50 & Target

IC50: 2.7 nM (mineralocorticoid receptor), 310 nM (progesterone receptor)[1]

In Vivo

PF-3882845 reduces blood pressure, decreases urinary albumin, and protects kidney in Dahl SS rat[1].
PF-3882845 exhibits moderate oral bioavailability (F 86%) following oral administration (2 mg/kg) in male Sprague-Dawley rats[1].
PF-3882845 exhibits terminal elimination half-lives (T1/2 1.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (Vdss 1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats[1].

Animal Model: Male Dahl salt sensitive (SS) rats[1]
Dosage: 10, 40, and 100 mg/kg
Administration: Orally via gavage; twice a day; for 21 days
Result: Significant blood pressure reduction was observed with 10 mg/kg. Most noticeably, rats dosed at 40 and 100 mg/kg had negligible increase in blood pressure over 21 days in the presence of high salt.
Molecular Weight

419.90

Formula

C₂₄H₂₂ClN₃O₂

CAS No.

1023650-66-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PF-3882845PF3882845PF 3882845Mineralocorticoid ReceptorProgesterone ReceptorNR3C3hypertensionnephropathyInhibitorinhibitorinhibit

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PF-3882845
Cat. No.:
HY-12738
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