PF-3882845
Based on 1 Customer Validation
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.
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- Pureza: 99.90%
- No. CAS: 1023650-66-9
- Fòrmula: C24H22ClN3O2
- Peso molecular:419.90
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
IC50: 2.7 nM (mineralocorticoid receptor), 310 nM (progesterone receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | IC50 |
21 nM
Compound: cis-27d
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Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
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[PMID: 20672822] |
| Huh-7 | IC50 |
9 nM
Compound: 3S,3aR-27d, PF-3882845
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Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
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[PMID: 20672822] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Dahl salt sensitive (SS) rats[1]
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Dosage:10, 40, and 100 mg/kg
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Administration:Orally via gavage; twice a day; for 21 days
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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.
Chemical Information
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No. CAS 1023650-66-9
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Appearance Solid
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Peso molecular 419.90
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Fòrmula C24H22ClN3O2
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Color Light yellow to yellow
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SMILES
N#CC1=CC=C(N2N=C(C(C=CC(C(O)=O)=C3)=C3CC4)[C@H]4[C@@H]2C5CCCC5)C=C1Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvente y solubilidad
DMSO : 10 mg/mL (23.82 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3815 mL | 11.9076 mL | 23.8152 mL | 59.5380 mL |
| 5 mM | 0.4763 mL | 2.3815 mL | 4.7630 mL | 11.9076 mL | |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3815 mL | 5.9538 mL | |
| 15 mM | 0.1588 mL | 0.7938 mL | 1.5877 mL | 3.9692 mL | |
| 20 mM | 0.1191 mL | 0.5954 mL | 1.1908 mL | 2.9769 mL |
PF-3882845 Related Classifications
HY-12738 Related Classifications
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