A non-steroidal mineralocorticoid receptor antagonist
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PF-03882845

Item No. 10669

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3S,3aR,4,5-tetrahydro-2H-benz[g]indazole-7-carboxylic acid
CAS Number
1023650-66-9
Molecular Formula
C24H22ClN3O2
Formula Weight
419.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
ClC1=CC(N2[C@@H](C3CCCC3)[C@H]4CCC5=CC(C(O)=O)=CC=C5C4=N2)=CC=C1C#N
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PF-03882845 is a non-steroidal mineralocorticoid receptor antagonist (IC50 = 26 nM).1 It is selective for the mineralocorticoid receptor over the androgen, glucocorticoid, and progesterone receptors in reporter assays using Huh7 cells (IC50s = >10,000, >10,000, and 1,880 nM, respectively). PF-03882845 (40 and 100 mg/kg) prevents blood pressure increases and kidney damage in rats fed a high-salt diet. It inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) guanine-N7 methyltransferase in a homogenous time-resolved fluorescence (HTRF) assay (IC50 = 1.1 µM) and reduces SARS-CoV-2 infectivity in Vero E6 cells (EC50 = 10.97 µM).2 PF-03882845 also inhibits Zika virus NS2B-NS3 protease in a reporter assay (IC50 = 1 µM) and reduces Zika virus infectivity in neural stem cells generated from human induced pluripotent stem cells (iPSCs; IC50 = 10.8 µM).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Meyers, M.J., Arhancet, G.B., Hockerman, S.L., 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. 53(16), 5979-6002 (2010).

    2. Basu, S., Mak, T., Ulferts, R., et al. Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp14 RNA cap methyltransferase. Biochem. J. 478(13), 2481-2497 (2021).

    3. Abrams, R.P.M., Yasgar, A., Teramoto, T., et al. Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. Proc. Natl. Acad. Sci. USA 117(49), 31365-31375 (2020).