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Terlakiren

Cat. No. M42603
Terlakiren Structure
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Biological Activity

Terlakiren (CP-80,794) is an orally active inhibitor of renin.

Chemical Information
Molecular Weight 620.8
Formula C31H48N4O7S
CAS Number 119625-78-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Serdar Durdagi et al. Mol Inform. Screening of Clinically Approved and Investigation Drugs as Potential Inhibitors of SARS-CoV-2: A Combined in silico and in vitro Study

[2] M L Mangiapane et al. Clin Exp Hypertens. Role of nitric oxide in responses to renin-angiotensin system inhibition in sodium-depleted guinea pig and rat

[3] R P Shannon et al. Cardiovasc Res. Effects of renin inhibition compared to angiotensin converting enzyme inhibition in conscious dogs with pacing-induced heart failure

[4] D J Hoover et al. Adv Exp Med Biol. Discovery of inhibitors of human renin with high oral bioavailability

[5] A A Fossa et al. J Cardiovasc Pharmacol. Synergistic effect on reduction in blood pressure with coadministration of the renin inhibitor, CP-80,794, and the angiotensin converting enzyme inhibitor, captopril

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  Catalog
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Keywords: Terlakiren supplier, Renin, inhibitors, activators


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