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Clazosentan

Chemical Structure : Clazosentan

CAS No.: 180384-56-9

Clazosentan (Ro 61-1790, VML 588, AXV-034343)

Catalog No.: PC-23409Not For Human Use, Lab Use Only.

Clazosentan (Ro 61-1790) is a potent, selective endothelin A (ETA) receptor antagonist, 1000-fold selectivity for the ETA over ETB receptor on functional assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Clazosentan (Ro 61-1790) is a potent, selective endothelin A (ETA) receptor antagonist, 1000-fold selectivity for the ETA over ETB receptor on functional assays.
Clazosentan (Ro 61-1790) inhibits contraction induced by ET-1 on isolated rat aorta (ETA receptors; pA2 = 9.5) or by sarafotoxin S6c on rat trachea (ETB receptors; pA2 = 6.4).
Clazosentan (Ro 61-1790) inhibited the pressor effect of big ET-1 in pithed rats with an ID50 value of 0.05 mg/kg.
Clazosentan (Ro 61-1790) both prevented and reversed cerebral vasospasm in a dose-dependent manner in double-hemorrhage canine model of SAH.

Physicochemical Properties

M.Wt 577.58
Formula C25H23N9O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-methylpyridine-2-sulfonamide

References

1. Roux S, et al. J Pharmacol Exp Ther. 1997 Dec;283(3):1110-8.

2. Okajima M, et al. Am J Physiol Heart Circ Physiol. 2004 Oct;287(4):H1476-83.

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