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IRL-1038

Cat. No. M40490
IRL-1038 Structure
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Biological Activity

IRL-1038 is a selective endothelin receptor ETB antagonist for studies related to cardiovascular disease.

Chemical Information
Molecular Weight 1409.67
Formula C68H92N14O15S2
CAS Number 144602-02-8
Form Solid
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] H Karaki et al. Eur J Pharmacol. ETB receptor antagonist, IRL 1038, selectively inhibits the endothelin-induced endothelium-dependent vascular relaxation

[2] H Karaki et al. Br J Pharmacol. Induction of endothelium-dependent relaxation in the rat aorta by IRL 1620, a novel and selective agonist at the endothelin ETB receptor

[3] Y Urade et al. FEBS Lett. An endothelin B receptor-selective antagonist: IRL 1038, [Cys11- Cys15]-endothelin-1(11-21)

[4] Y Fujitani et al. J Pharmacol Exp Ther. A selective agonist of endothelin type B receptor, IRL 1620, stimulates cyclic GMP increase via nitric oxide formation in rat aorta

[5] Y Urade et al. FEBS Lett. An endothelin B receptor-selective antagonist: IRL 1038, [Cys11-Cys15]-endothelin-1(11-21)

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Keywords: IRL-1038 supplier, Endothelin Receptor, inhibitors, activators

 
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