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ET receptor antagonist 3

Cat. No. M43592
ET receptor antagonist 3 Structure
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Biological Activity

ET receptor antagonist 3 is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH).

Chemical Information
Molecular Weight 548.61
Formula C27H28N6O5S
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] J K Prague et al. Climacteric. Neurokinin 3 receptor antagonism - the magic bullet for hot flushes?

[2] Mostafa M Elgebaly et al. Vascul Pharmacol. Differential effects of ET(A) and ET(B) receptor antagonism on oxidative stress in type 2 diabetes

[3] Paul Neary et al. Expert Opin Investig Drugs. Alvimopan

[4] Masayasu Takahashi et al. CNS Drug Rev. YM872: a selective, potent and highly water-soluble alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist

[5] C Martin et al. Naunyn Schmiedebergs Arch Pharmacol. Differential effects of the mixed ET(A)/ET(B)-receptor antagonist bosentan on endothelin-induced bronchoconstriction, vasoconstriction and prostacyclin release

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Keywords: ET receptor antagonist 3 supplier, Estrogen Receptor, inhibitors, activators


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