H-77
H-77 is a selective Renin inhibitor with an IC50 of 1.2 μM. H-77 causes dose-dependent decreases in plasma angiotensin I, plasma angiotensin II, and mean arterial pressure in sodium-depleted conscious beagle dogs. H-77 does not alter blood pressure or plasma angiotensin II levels in conscious chronically cannulated rats. H-77 can be used in studies related to the physiological and pathological states of the renin-angiotensin system.
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- CAS No.: 82131-82-6
- Formule: C52H74N12O9
- Masse moléculaire:1011.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
H-77 (1.0-10.0 mg/kg; intravenous injection) does not significantly alter the mean arterial pressure or plasma angiotensin II concentration in conscious, unrestrained female Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle (male, 12.7-18 kg, sodium-depleted hypertension model)[1]
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Dosage:0.01 mg·kg-1·hr-1; 0.1 mg·kg-1·hr-1; 1.0 mg·kg-1·hr-1; 10.0 mg·kg-1·hr-1
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Administration:i.v.; 30 minutes (0.01, 1.0, 10.0 mg·kg-1·hr-1); 4 hours (0.1 mg·kg-1·hr-1)
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Result:Reduced circulating angiotensin I and angiotensin II concentrations within 15 minutes, with effects persisting through the 4-hour infusion, and lowered mean arterial pressure at 0.1 mg·kg-1·hr-1.
Markedly reduced plasma angiotensin I and angiotensin II concentrations, with significant decreases relative to control (p < 0.01 to p < 0.001) at 1.0 and 10.0 mg·kg-1·hr-1.
Produced greater, more persistent reductions in mean arterial pressure, with heart rate increasing significantly during marked hypotension from the 10.0 mg·kg-1·hr-1 dose.
Had little effect on angiotensin levels or blood pressure at 0.01 mg·kg-1·hr-1.
Correlated significantly between changes in plasma angiotensin II concentration and changes in angiotensin I concentration (r = 0.72-0.77, p < 0.001) and mean arterial pressure (r = 0.69-0.72, p < 0.001).
Chemical Information
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CAS No. 82131-82-6
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Masse moléculaire 1011.24
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Formule C52H74N12O9
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SMILES
C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC2=CN=CN2)C(N[C@H](CN[C@H](C(N[C@H](C(N[C@@H](CC3=CC=C(O)C=C3)C(O)=O)=O)C(C)C)=O)CC(C)C)CC(C)C)=O)=O)(=O)[C@H]4N(C([C@@H](CC5=CN=CN5)N)=O)CCC4
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Sequence
His-Pro-Phe-His-{Leu(CH2-NH)}-Leu-Val-Tyr
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Sequence Shortening
HPFH-{Leu(CH2-NH)}-LVY
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Szelke M, et al. H-77: a potent new renin inhibitor. In vitro and in vivo studies. Hypertension (Dallas, Tex. : 1979). 1982;4(3 Pt 2):59-69. [Content Brief]
[2]. LECKIE B J, et al. Human renin inhibitors[J]. 1985.
[3]. McIntyre GD, et al. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
H-77 Related Classifications
HY-P2647 Related Classifications
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