PZ0031

PF-03882845

≥98% (HPLC)

• Synonym(s): (3S,3aR)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid, PF-3882845
• Empirical Formula (Hill Notation): C₂₄H₂₂ClN₃O₂
• CAS Number: 1023650-66-9
• Molecular Weight: 419.90
• MDL number: MFCD28124394
• UNSPSC Code: 51111800
• PubChem Substance ID: 329823690
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: room temp
• SMILES string: OC(C1=CC2=C(C=C1)C3=NN(C4=CC=C(C#N)C(Cl)=C4)[C@@H](C5CCCC5)[C@@]3([H])CC2)=O
• InChI: 1S/C24H22ClN3O2/c25-21-12-18(8-5-17(21)13-26)28-23(14-3-1-2-4-14)20-10-6-15-11-16(24(29)30)7-9-19(15)22(20)27-28/h5,7-9,11-12,14,20,23H,1-4,6,10H2,(H,29,30)/t20-,23-/m0/s1
• InChI key: XNULRSOGWPFPBL-REWPJTCUSA-N

Description

Biochem/physiol Actions

PF-03882845 is a potent non-steroidal mineralocorticoid antagonist with and IC₅₀ of 0.755 nM, compared to eplerenone with an IC₅₀ of 109 nM. PF-03882845 was tested in a rat model for renal protection against aldosterone-mediated renal disease, and found to be more potent than eplerenone in suppressing the urinary albumin to creatinine ratio (UACR), a measure of renal fibrosis. The therapeutic index, calculated as the ratio of the EC₅₀ for increasing serum K+ to the EC₅₀ for UACR lowering, was 83.8 for PF-03882845 and 1.47 for eplerenone.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319,H335
• pcodes: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable