2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. Mineralocorticoid Receptor Progesterone Receptor
  4. 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.

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]
Cellular Effect
Cell Line Type Value Description References
Huh-7 IC50
21 nM
Compound: cis-27d
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
[PMID: 20672822]
Huh-7 IC50
9 nM
Compound: 3S,3aR-27d, PF-3882845
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
[PMID: 20672822]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3815 mL 11.9076 mL 23.8152 mL
5 mM 0.4763 mL 2.3815 mL 4.7630 mL
View the 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.9%

SDS (393 KB)

COA (253 KB)

Handling Instructions (2659 KB)
References

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
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PF-3882845 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-38828451023650-66-9PF3882845PF 3882845Mineralocorticoid ReceptorProgesterone ReceptorNR3C3hypertensionnephropathyInhibitorinhibitorinhibit

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