WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 598050
CAS#: 82131-82-6
Description: H 77 is a potent new renin inhibitor. H 77 is an angiotensinogen (6-13)-octapeptide in which the peptide bond -CO-NH- at the Leu(9)-Leu(11) linkage is replaced by a -CH2-NH- bond.
MedKoo Cat#: 598050
Name: H 77
CAS#: 82131-82-6
Chemical Formula: C52H74N12O9
Exact Mass: 1010.5702
Molecular Weight: 1011.23
Elemental Analysis: C, 61.76; H, 7.38; N, 16.62; O, 14.24
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Synonym: H 77; H-77; H77;
IUPAC/Chemical Name: ((S)-2-((S)-2-((S)-2-((S)-1-(D-histidyl)pyrrolidine-2-carboxamido)-3-phenylpropanamido)-3-(1H-imidazol-4-yl)propanamido)-4-methylpentyl)-L-leucyl-L-valyl-L-tyrosine
InChi Key: ABDWINSTWUZFIV-RLWIUDPYSA-N
InChi Code: InChI=1S/C52H74N12O9/c1-30(2)19-37(27-56-40(20-31(3)4)46(66)63-45(32(5)6)50(70)62-43(52(72)73)22-34-14-16-38(65)17-15-34)59-47(67)42(24-36-26-55-29-58-36)60-48(68)41(21-33-11-8-7-9-12-33)61-49(69)44-13-10-18-64(44)51(71)39(53)23-35-25-54-28-57-35/h7-9,11-12,14-17,25-26,28-32,37,39-45,56,65H,10,13,18-24,27,53H2,1-6H3,(H,54,57)(H,55,58)(H,59,67)(H,60,68)(H,61,69)(H,62,70)(H,63,66)(H,72,73)/t37-,39+,40-,41-,42-,43-,44-,45-/m0/s1
SMILES Code: OC1=CC=C(C=C1)C[C@@H](C(O)=O)NC([C@H](C(C)C)NC([C@H](CC(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)N)=O)CCC4)=O)=O)=O)CC(C)C)=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 1011.23 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: Szelke M, Leckie BJ, Tree M, Brown A, Grant J, Hallett A, Hughes M, Jones DM, Lever AF. H-77: a potent new renin inhibitor. In vitro and in vivo studies. Hypertension. 1982 May-Jun;4(3 Pt 2):59-69. PubMed PMID: 7040240.
2: McIntyre GD, Leckie B, Hallett A, Szelke M. Purification of human renin by affinity chromatography using a new peptide inhibitor of renin, H.77 (D-His-Pro-Phe-His-LeuR-Leu-Val-Tyr). Biochem J. 1983 May 1;211(2):519-22. PubMed PMID: 6347189; PubMed Central PMCID: PMC1154389.
3: Tree M, Fraser R, Holloway C, Hughes M, Ingram M, Leckie BJ, Lever AF, Morton JJ, Szelke M. Role of renin as a blood-borne hormone tested by infusion of renin inhibitor (H.77). Kidney Int Suppl. 1988 Sep;25:S33-7. PubMed PMID: 3054239.
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: De Godoy MA, Rattan S. Autocrine regulation of internal anal sphincter tone by renin-angiotensin system: comparison with phasic smooth muscle. Am J Physiol Gastrointest Liver Physiol. 2005 Dec;289(6):G1164-75. Epub 2005 Jul 14. PubMed PMID: 16020656.
6: Oldham AA, Arnstein MJ, Major JS, Clough DP. Effects of the renin inhibitor H77 on the pressor responses to injected pig, rat and dog renins in vivo. J Hypertens. 1983 Aug;1(2):191-5. PubMed PMID: 6397517.
7: Müller-Schweinitzer E. Interaction of cyclosporine-A with the renin-angiotensin system in canine veins. Naunyn Schmiedebergs Arch Pharmacol. 1989 Aug;340(2):252-7. PubMed PMID: 2682268.
8: Tree M, MacArthur K, Inglis G, Leckie B, Lever AF, Morton JJ, Szelke M. Effects of the renin inhibitor H77 on angiotensin II, arterial pressure and cardiac function in conscious dogs: comparison with captopril. J Hypertens Suppl. 1989 Apr;7(2):S51-5. PubMed PMID: 2666615.
9: Papaioannou S, Hansen D Jr, Babler M, Yang PC, Bittner S, Miller A, Clare M. New class of inhibitors specific for human renin. Clin Exp Hypertens A. 1985;7(9):1243-57. PubMed PMID: 3000656.
10: Tonolo G, Tree M, Pazzola A, Leckie BJ. Similarity between active and trypsin-activated inactive renin in dog plasma by means of renin inhibition: the dog as an animal model for studies of inactive renin. J Hypertens. 1988 Dec;6(12):975-80. PubMed PMID: 3065412.
11: 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.
12: Song K, Zhuo J, Chai SY, Mendelsohn FA. A new method to localize active renin in tissues by autoradiography: application to dog kidney. Kidney Int. 1992 Sep;42(3):639-46. PubMed PMID: 1405342.
13: Hofbauer KG, Wood JM. Inhibition of renin: recent developments. Contrib Nephrol. 1984;43:144-52. Review. PubMed PMID: 6207982.
14: Oldham AA, Arnstein MJ, Major JS, Clough DP. In vivo comparison of the renin inhibitor H77 with the angiotensin-converting enzyme inhibitor captopril. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):672-7. PubMed PMID: 6206324.
15: Schwieler JH, Nussberger J, Kahan T, Hjemdahl P. Angiotensin II overflow from canine skeletal muscle in vivo: importance of plasma angiotensin I. Am J Physiol. 1994 May;266(5 Pt 2):R1664-9. PubMed PMID: 8203648.
16: Zhuo J, Anderson WP, Song K, Mendelsohn FA. Autoradiographic localization of active renin in the juxtaglomerular apparatus of the dog kidney: effects of sodium intake. Clin Exp Pharmacol Physiol. 1996 Apr;23(4):291-8. PubMed PMID: 8717064.