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RES-701-1

Cat. No. M40487
RES-701-1 Structure
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Biological Activity

RES-701-1 is an endothelin receptor ETB antagonist that can be used in studies related to cardiovascular disease.

Chemical Information
Molecular Weight 2043.16
Formula C103H115N23O23
CAS Number 151308-34-8
Storage −20°C
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] K Shibata et al. Bioorg Med Chem. Hybrid peptides constructed from RES-701-1, an endothelin B receptor antagonist, and endothelin; binding selectivity for endothelin receptors and their pharmacological activity

[2] T Ikemura et al. J Pharm Pharmacol. Effects of endothelin B antagonist RES-701-1 on endothelin-induced contractile responses in-vivo and in-vitro in guinea-pigs

[3] T Tanaka et al. Mol Pharmacol. RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin

[4] Y Morishita et al. J Antibiot (Tokyo). RES-701-1, a novel and selective endothelin type B receptor antagonist produced by Streptomyces sp. RE-701. I. Characterization of producing strain, fermentation, isolation, physico-chemical and biological properties

[5] T Tanaka et al. Biochem Biophys Res Commun. Species difference in the binding characteristics of RES-701-1: potent endothelin ETB receptor-selective antagonist

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Keywords: RES-701-1 supplier, Endothelin Receptor, inhibitors, activators

 
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