WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H525939
CAS#: 1023650-66-9
Description: PF-03882845 is a highly potent (IC50=6.3‐13.4nM,10% fetal bovine serum & IC50= 0.504–1.11 nM, absence of serum) selective orally bioavailable mineralocorticoid receptor antagonist. It prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy.
Hodoodo Cat#: H525939
Name: PF-03882845
CAS#: 1023650-66-9
Chemical Formula: C24H22ClN3O2
Exact Mass: 419.14
Molecular Weight: 419.909
Elemental Analysis: C, 68.65; H, 5.28; Cl, 8.44; N, 10.01; O, 7.62
Synonym: PF-03882845; PF 03882845; PF03882845.
IUPAC/Chemical Name: (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid
InChi Key: XNULRSOGWPFPBL-REWPJTCUSA-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
SMILES Code: O=C(C1=CC=C2C(CC[C@]3([H])[C@H](C4CCCC4)N(C5=CC=C(C#N)C(Cl)=C5)N=C23)=C1)O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 419.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Kolkhof P, Nowack C, Eitner F. Nonsteroidal antagonists of the mineralocorticoid receptor. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):417-24. doi: 10.1097/MNH.0000000000000147. Review. PubMed PMID: 26083526.
2: Bisping E, Wakula P, Poteser M, Heinzel FR. Targeting cardiac hypertrophy: toward a causal heart failure therapy. J Cardiovasc Pharmacol. 2014 Oct;64(4):293-305. doi: 10.1097/FJC.0000000000000126. Review. PubMed PMID: 25286359.
3: Fryer RM, Boustany-Kari CM, MacDonnell SM. Engaging novel cell types, protein targets and efficacy biomarkers in the treatment of diabetic nephropathy. Front Pharmacol. 2014 Aug 7;5:185. doi: 10.3389/fphar.2014.00185. eCollection 2014. PubMed PMID: 25147524; PubMed Central PMCID: PMC4124518.
4: Casimiro-Garcia A, Piotrowski DW, Ambler C, Arhancet GB, Banker ME, Banks T, Boustany-Kari CM, Cai C, Chen X, Eudy R, Hepworth D, Hulford CA, Jennings SM, Loria PM, Meyers MJ, Petersen DN, Raheja NK, Sammons M, She L, Song K, Vrieze D, Wei L. Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-me thoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist. J Med Chem. 2014 May 22;57(10):4273-88. doi: 10.1021/jm500206r. Epub 2014 Apr 30. PubMed PMID: 24738581.
5: Orena S, Maurer TS, She L, Eudy R, Bernardo V, Dash D, Loria P, Banker ME, Tugnait M, Okerberg CV, Qian J, Boustany-Kari CM. PF-03882845, a non-steroidal mineralocorticoid receptor antagonist, prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy. Front Pharmacol. 2013 Oct 14;4:115. doi: 10.3389/fphar.2013.00115. eCollection 2013. PubMed PMID: 24133446; PubMed Central PMCID: PMC3796291.
6: Eudy RJ, Sahasrabudhe V, Sweeney K, Tugnait M, King-Ahmad A, Near K, Loria P, Banker ME, Piotrowski DW, Boustany-Kari CM. The use of plasma aldosterone and urinary sodium to potassium ratio as translatable quantitative biomarkers of mineralocorticoid receptor antagonism. J Transl Med. 2011 Oct 21;9:180. doi: 10.1186/1479-5876-9-180. PubMed PMID: 22017794; PubMed Central PMCID: PMC3305907.
