WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 597553
CAS#: 85139-12-4
Description: H 142 is a decapeptide inhibitor of human renin.
MedKoo Cat#: 597553
Name: H 142
CAS#: 85139-12-4
Chemical Formula: C60H91N17O10
Exact Mass: 1209.7135
Molecular Weight: 1210.49
Elemental Analysis: C, 59.53; H, 7.58; N, 19.67; O, 13.22
This product is not in stock, which may be available by custom synthesis.
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Synonym: H 142; H-142; H142;
IUPAC/Chemical Name: ((S)-2-((S)-2-((S)-2-((S)-1-(L-prolyl-L-histidyl)pyrrolidine-2-carboxamido)-3-phenylpropanamido)-3-(1H-imidazol-4-yl)propanamido)-4-methylpentyl)-L-valyl-L-isoleucyl-L-histidyl-L-lysine
InChi Key: XIZSMQBWVQNHCA-NIRMQQKASA-N
InChi Code: InChI=1S/C60H91N17O10/c1-7-37(6)51(58(84)74-47(26-40-29-63-33-68-40)55(81)71-44(60(86)87)17-11-12-20-61)76-57(83)50(36(4)5)66-31-42(23-35(2)3)70-53(79)46(25-39-28-62-32-67-39)72-54(80)45(24-38-15-9-8-10-16-38)73-56(82)49-19-14-22-77(49)59(85)48(27-41-30-64-34-69-41)75-52(78)43-18-13-21-65-43/h8-10,15-16,28-30,32-37,42-51,65-66H,7,11-14,17-27,31,61H2,1-6H3,(H,62,67)(H,63,68)(H,64,69)(H,70,79)(H,71,81)(H,72,80)(H,73,82)(H,74,84)(H,75,78)(H,76,83)(H,86,87)/t37-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-/m0/s1
SMILES Code: NCCCC[C@@H](C(O)=O)NC([C@H](CC1=CNC=N1)NC([C@H]([C@@H](C)CC)NC([C@H](C(C)C)NC[C@@H](NC([C@H](CC2=CNC=N2)NC([C@H](CC3=CC=CC=C3)NC([C@H]4N(C([C@H](CC5=CNC=N5)NC([C@H]6NCCC6)=O)=O)CCC4)=O)=O)=O)CC(C)C)=O)=O)=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: >3 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: 2934.99.03.00
The following data is based on the product molecular weight 1210.49 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: Webb DJ, Cumming AM, Leckie BJ, Lever AF, Morton JJ, Robertson JI, Szelke M, Donovan B. Reduction of blood pressure in man with H-142, a potent new renin inhibitor. Lancet. 1983 Dec 24-31;2(8365-66):1486-7. PubMed PMID: 6140568.
2: Tree M, Atrash B, Donovan B, Gamble J, Hallett A, Hughes M, Jones DM, Leckie B, Lever AF, Morton JJ, et al. New inhibitors of human renin tested in vitro and in vivo in the anaesthetized baboon. J Hypertens. 1983 Dec;1(4):399-403. PubMed PMID: 6398331.
3: Hofbauer KG, Ménard J, Michel JB, Wood JM. Inhibition of renin in the primate Callithrix jacchus (common marmoset). Clin Exp Hypertens A. 1983;5(7-8):1237-47. PubMed PMID: 6196144.
4: Tree M, Szelke M, Leckie B, Atrash B, Donovan B, Hallett A, Jones DM, Lever AF, Morton JJ, Sueiras-Diaz J, et al. Renin inhibitors: their use in understanding the role of angiotensin II as a pressor hormone. J Cardiovasc Pharmacol. 1985;7 Suppl 4:S49-52. PubMed PMID: 2412013.
5: Foundling SI, Cooper J, Watson FE, Cleasby A, Pearl LH, Sibanda BL, Hemmings A, Wood SP, Blundell TL, Valler MJ, et al. High resolution X-ray analyses of renin inhibitor-aspartic proteinase complexes. Nature. 1987 May 28-Jun 3;327(6120):349-52. PubMed PMID: 3295561.
6: Gómez J, Semo N, Freire E. Structural thermodynamic study of the binding of renin inhibitors to endothiapepsin. Adv Exp Med Biol. 1998;436:325-8. PubMed PMID: 9561236.
7: Movahedi S, Norey CG, Kay J, Heale JB. Infection and pathogenesis of cash crops by Botrytis cinerea: primary role of an aspartic proteinase. Adv Exp Med Biol. 1991;306:213-6. PubMed PMID: 1812708.
8: Teleman O, Lindberg M, Engström S. Molecular dynamics simulation of the renin inhibitor H142 in water. J Comput Aided Mol Des. 1991 Jun;5(3):187-203. PubMed PMID: 1919616.
9: Webb DJ, Manhem PJ, Ball SG, Inglis G, Leckie BJ, Lever AF, Morton JJ, Robertson JI, Murray GD, Ménard J, et al. A study of the renin inhibitor H142 in man. J Hypertens. 1985 Dec;3(6):653-8. PubMed PMID: 3910726.
10: Webb DJ, Manhem PJ, Ball SG, Inglis G, Leckie BJ, Lever AF, Morton JJ, Robertson JI, Murray GD, Ménard J, et al. Clinical and biochemical effects of the renin inhibitor H142 in humans. J Cardiovasc Pharmacol. 1987;10 Suppl 7:S69-74. PubMed PMID: 2485066.
11: Webb DJ, Manhem PJ, Leckie BJ, Lever AJ, Morton JJ, Robertson JI, Semple PF, Szelke M. Severe hypotension with bradycardia during renin inhibition with H142 in sodium deplete man. J Hum Hypertens. 1989 Aug;3(4):227-32. PubMed PMID: 2677374.
12: Hofbauer KG, Fuhrer W, Heusser C, Wood JM. Comparison of different drug interference with the renin-angiotensin system. J Cardiovasc Pharmacol. 1985;7 Suppl 4:S62-8. PubMed PMID: 2412016.
13: Cooper JB, Foundling SI, Hemmings A, Watson FE, Sibanda BL, Blundell TL, Jones DM, Hallett A, Atrash B, Szelke M. Inhibitors of aspartic proteinases and their relevance to the design of antihypertensive agents. Biochem Soc Trans. 1987 Aug;15(4):751-4. PubMed PMID: 3119394.
14: Hofbauer KG, Wood JM. Inhibition of renin: recent developments. Contrib Nephrol. 1984;43:144-52. Review. PubMed PMID: 6207982.
