Synonym
Kri 1314; Kri1314; Kri-1314
IUPAC/Chemical Name
Cyclohexanebutanoic acid, alpha-hydroxy-beta-((3-(1H-imidazol-4-yl)-2-((4-(4-morpholinyl)-2-(1-naphthalenylmethyl)-1,4-dioxobutyl)amino)-1-oxopropyl)amino)-, 1-methylethyl ester
InChi Key
NQXSBCTYTMQGGJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C38H51N5O7/c1-25(2)50-38(48)35(45)32(19-26-9-4-3-5-10-26)41-37(47)33(22-30-23-39-24-40-30)42-36(46)29(21-34(44)43-15-17-49-18-16-43)20-28-13-8-12-27-11-6-7-14-31(27)28/h6-8,11-14,23-26,29,32-33,35,45H,3-5,9-10,15-22H2,1-2H3,(H,39,40)(H,41,47)(H,42,46)
SMILES Code
O=C(OC(C)C)C(O)C(NC(C(NC(C(CC1=C2C=CC=CC2=CC=C1)CC(N3CCOCC3)=O)=O)CC4=CNC=N4)=O)CC5CCCCC5
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
689.85
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: Etoh Y, Miyazaki M, Saitoh H, Toda N. KRI-1314: an orally effective inhibitor of human renin. Jpn J Pharmacol. 1993 Sep;63(1):109-19. doi: 10.1254/jjp.63.109. PMID: 8271523.
2: Saitoh H, Etoh Y, Murakami M, Kubota T, Miyazaki M. [Hypotensive action of human renin inhibitor KRI-1314 in the common marmoset]. Nihon Yakurigaku Zasshi. 1994 Apr;103(4):161-73. Japanese. doi: 10.1254/fpj.103.161. PMID: 8175079.
3: Miyazaki M, Etoh Y, Iizuka K, Toda N. An orally active renin inhibitor: cyclohexylnorstatine-containing dipeptide (KRI-1314). J Hypertens Suppl. 1989 Apr;7(2):S25-7. PMID: 2666609.
4: Mizuno K, Niimura S, Tani M, Haga H, Inagami T, Fukuchii S. Direct proof for local generation and release of angiotensin II in peripheral human vascular tissue. Am J Hypertens. 1991 Jan;4(1 Pt 2):67S-72S. doi: 10.1093/ajh/4.1.67s. PMID: 2009152.
5: Shibasaki M, Sudoh K, Asano M, Murakami K. The effect of intravenous recombinant human renin on blood pressure in pithed spontaneously hypertensive rats. Eur J Pharmacol. 1992 May 14;215(2-3):271-6. doi: 10.1016/0014-2999(92)90038-6. PMID: 1396991.
6: Shibasaki M, Asano M, Fukunaga Y, Usui T, Ichihara M, Murakami Y, Nakano K, Fujikura T. Pharmacological properties of YM-21095, a potent and highly specific renin inhibitor. Am J Hypertens. 1991 Dec;4(12 Pt 1):932-8. doi: 10.1093/ajh/4.12.932. PMID: 1815649.
7: Salimbeni A, Paleari F, Poma D, Criscuoli M, Scolastico C. Synthesis and renin inhibitory activity of novel angiotensinogen transition state analogues modified at the P(2)-histidine position. Eur J Med Chem. 1996;31(10):827-32. doi: 10.1016/0223-5234(96)83977-8. PMID: 22026939.
8: Iizuka K, Kamijo T, Harada H, Akahane K, Kubota T, Umeyama H, Ishida T, Kiso Y. Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction. J Med Chem. 1990 Oct;33(10):2707-14. doi: 10.1021/jm00172a005. PMID: 2120440.
9: Okamura T, Wang Y, Toda N. Local generation and action of angiotensin II in dog iris sphincter muscle. Exp Eye Res. 1992 Oct;55(4):563-8. doi: 10.1016/s0014-4835(05)80169-1. PMID: 1336465.
