Synonym
SR 42128; SR-42128; SR42128;
IUPAC/Chemical Name
(3S,12S,14S,16S,18S)-18-benzyl-14-carbamoyl-16-ethyl-3,11-dihydroxy-4,12-diisobutyl-7,22-dimethyl-6,9,17,20-tetraoxo-5,8,13,19-tetraazatricosanoic acid
InChi Key
IVNZELLFTLZSGY-MCQYDUJISA-N
InChi Code
InChI=1S/C39H65N5O9/c1-9-27(37(51)30(43-34(47)17-24(6)7)18-26-13-11-10-12-14-26)19-31(38(40)52)42-28(15-22(2)3)32(45)20-35(48)41-25(8)39(53)44-29(16-23(4)5)33(46)21-36(49)50/h10-14,22-25,27-33,42,45-46H,9,15-21H2,1-8H3,(H2,40,52)(H,41,48)(H,43,47)(H,44,53)(H,49,50)/t25?,27-,28-,29?,30-,31-,32?,33-/m0/s1
SMILES Code
CC[C@H](C([C@H](CC1=CC=CC=C1)NC(CC(C)C)=O)=O)C[C@@H](C(N)=O)N[C@@H](CC(C)C)C(O)CC(NC(C)C(NC([C@@H](O)CC(O)=O)CC(C)C)=O)=O
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
747.97
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: Delie F, Couvreur P, Nisato D, Michel JB, Puisieux F, Letourneux Y. Synthesis and in vitro study of a diglyceride prodrug of a peptide. Pharm Res. 1994 Aug;11(8):1082-7. PubMed PMID: 7971705.
2: Cumin F, Nisato D, Gagnol JP, Corvol P. A potent radiolabeled human renin inhibitor, [3H]SR42128: enzymatic, kinetic, and binding studies to renin and other aspartic proteases. Biochemistry. 1987 Dec 1;26(24):7615-21. PubMed PMID: 3322402.
3: Gougat J, Canat S, Lacour C, Cazaubon C, Gagnol J, Nisato D. [Increase in plasma levels of active and inactive renin after inhibition of renin activity by SR 42128 in conscious Macaca monkeys]. Arch Mal Coeur Vaiss. 1987 Jun;80(6):875-8. French. PubMed PMID: 3116988.
4: Chansel D, Dussaule JC, Ardaillou N, Ardaillou R. Identification and regulation of renin in human cultured mesangial cells. Am J Physiol. 1987 Jan;252(1 Pt 2):F32-8. PubMed PMID: 3544867.
5: Serre M, Galindo G, Marion A, Lacour C, Cazaubon C, Gagnol JP, Nisato D. Hemodynamic response to SR 42128A in normal and sodium-depleted baboons. J Cardiovasc Pharmacol. 1987;10 Suppl 7:S99-101. PubMed PMID: 2485074.
6: Cumin F, Nisato D, Gagnol JP, Corvol P. Binding of a tritiated pepstatin analog to human renin. J Cardiovasc Pharmacol. 1987;10 Suppl 7:S102-4. PubMed PMID: 2485039.
7: de Claviere M, Fourment P, Richaud JP, Unkovic J, Gagnol JP, Mazue G. Haemodynamic effects of the renin inhibitor SR 42128 in conscious baboons. J Hypertens Suppl. 1985 Dec;3(3):S271-3. PubMed PMID: 2856716.
8: De Claviere M, Cazaubon C, Lacour C, Nisato D, Gagnol JP, Evin G, Corvol P. In vitro and in vivo inhibition of human and primate renin by a new potent renin inhibitor: SR 42128. J Cardiovasc Pharmacol. 1985;7 Suppl 4:S58-61. PubMed PMID: 2412015.
