1023650-66-9
1023650-66-9 structure
- Name: PF-3882845
- Chemical Name: (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid
- CAS Number: 1023650-66-9
- Molecular Formula: C24H22ClN3O2
- Molecular Weight: 419.90300
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Mineralocorticoid Receptor
- Create Date: 2018-06-12 05:37:42
- Modify Date: 2024-01-02 17:59:56
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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].
| Name | (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acid |
|---|---|
| Synonyms |
unii-34zku73fu3
PF-03882845 |
| 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]. |
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| Related Catalog | |
| 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. |
| References |
| Molecular Formula | C24H22ClN3O2 |
|---|---|
| Molecular Weight | 419.90300 |
| Exact Mass | 419.14000 |
| PSA | 76.69000 |
| LogP | 4.75598 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |