Synonym
KBP-5074; KBP5074; KBP 5074;
IUPAC/Chemical Name
2-chloro-4-((3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidine-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl)benzonitrile
InChi Key
UXHQLGLGLZKHTC-CUNXSJBXSA-N
InChi Code
InChI=1S/C28H30ClN5O2/c29-23-15-19(6-5-18(23)16-30)34-27(17-3-1-2-4-17)22-8-9-24-21(26(22)32-34)7-10-25(31-24)28(36)33-13-11-20(35)12-14-33/h5-7,10,15,17,20,22,27,35H,1-4,8-9,11-14H2/t22-,27-/m0/s1
SMILES Code
ClC1=CC(N2[C@@H](C3CCCC3)[C@@H](CCC4=NC(C(N5CCC(O)CC5)=O)=CC=C46)C6=N2)=CC=C1C#N
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
504.03
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 |
1: Georgianos PI, Agarwal R. Management of hypertension in advanced kidney disease. Curr Opin Nephrol Hypertens. 2022 Jul 1;31(4):374-379. doi: 10.1097/MNH.0000000000000812. PMID: 35727171.
2: Al Dhaybi O, Bakris GL. Mineralocorticoid Receptor Antagonists-Evidence for Kidney Protection, Trials With Novel Agents. Adv Chronic Kidney Dis. 2021 Jul;28(4):371-377. doi: 10.1053/j.ackd.2021.07.005. PMID: 34922693.
3: Kintscher U, Bakris GL, Kolkhof P. Novel non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease. Br J Pharmacol. 2022 Jul;179(13):3220-3234. doi: 10.1111/bph.15747. Epub 2022 Jan 13. PMID: 34811750.
4: Barrera-Chimal J, Kolkhof P, Lima-Posada I, Joachim A, Rossignol P, Jaisser F. Differentiation between emerging non-steroidal and established steroidal mineralocorticoid receptor antagonists: head-to-head comparisons of pharmacological and clinical characteristics. Expert Opin Investig Drugs. 2021 Nov;30(11):1141-1157. doi: 10.1080/13543784.2021.2002844. Epub 2021 Dec 6. PMID: 34758679.
5: Pitt B, Jaisser F, Bakris G. An evaluation of KBP-5074 in advanced chronic kidney disease with uncontrolled hypertension. Expert Opin Investig Drugs. 2021 Oct;30(10):1017-1023. doi: 10.1080/13543784.2021.1985462. Epub 2021 Oct 19. PMID: 34595995.
6: Kolkhof P, Joseph A, Kintscher U. Nonsteroidal mineralocorticoid receptor antagonism for cardiovascular and renal disorders - New perspectives for combination therapy. Pharmacol Res. 2021 Oct;172:105859. doi: 10.1016/j.phrs.2021.105859. Epub 2021 Aug 28. PMID: 34461222.
7: Jaisser F, Tan X, Chi S, Liu J, Wang P, Bush M, Benn V, Yang YF, Zhang J. The Non-Steroidal Mineralocorticoid Receptor Antagonist KBP-5074 Limits Albuminuria and has Improved Therapeutic Index Compared With Eplerenone in a Rat Model With Mineralocorticoid-Induced Renal Injury. Front Pharmacol. 2021 Jun 24;12:604928. doi: 10.3389/fphar.2021.604928. PMID: 34248613; PMCID: PMC8264204.
8: Bakris G, Pergola PE, Delgado B, Genov D, Doliashvili T, Vo N, Yang YF, McCabe J, Benn V, Pitt B; BLOCK-CKD Study Group. Effect of KBP-5074 on Blood Pressure in Advanced Chronic Kidney Disease: Results of the BLOCK-CKD Study. Hypertension. 2021 Jul;78(1):74-81. doi: 10.1161/HYPERTENSIONAHA.121.17073. Epub 2021 May 10. PMID: 33966452; PMCID: PMC8189259.
9: Bakris G, Yang YF, Pitt B. Mineralocorticoid Receptor Antagonists for Hypertension Management in Advanced Chronic Kidney Disease: BLOCK-CKD Trial. Hypertension. 2020 Jul;76(1):144-149. doi: 10.1161/HYPERTENSIONAHA.120.15199. Epub 2020 Jun 10. PMID: 32520623.
