2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Renin Angiotensin Receptor
  4. 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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H-77

H-77 Chemical Structure

CAS No. : 82131-82-6

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H-77 Related Antibodies

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Description

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[1][2][3].

In Vitro

H-77 (Multiple concentrations) potently inhibits renin in human kidney extract with an IC50 of 1.2 μM, but is a weak inhibitor of renal acid protease with an IC50 of 3000 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

H-77 Related Antibodies
In Vivo

H-77 (0.005-5 mg/kg; 0.01-10.0 mg·kg-1·h-1; intravenous administration; 30 min-4 h) dose-dependently decreases plasma angiotensin I, plasma angiotensin II and mean arterial pressure in conscious sodium-depleted Beagle dogs, with a minimum effective dose of 0.1 mg·kg-1·hr-1[1].
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.

Animal Model: Beagle (male, 12.7-18 kg, sodium-depleted hypertension model)[1]
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
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)
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).
Molecular Weight

1011.24

Formula

C52H74N12O9
CAS No.
Sequence

His-Pro-Phe-His-{Leu(CH2-NH)}-Leu-Val-Tyr
Sequence Shortening

HPFH-{Leu(CH2-NH)}-LVY
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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H-77 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H-7782131-82-6H77H 77ReninAngiotensin Receptorhuman renincanine reninWistar ratshuman kidney cortex tissuerenal acid proteasesodium-depleted dogsangiotensin Iangiotensin IImean arterial pressurerat reninInhibitorinhibitorinhibit

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