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Clazosentan

$250$1,950

Products Details

Product Description

– Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction[1][5].

Web ID

– HY-17352

Storage Temperature

– -20°C, 3 years (Powder)

Shipping

– Blue Ice

Molecular Formula

– C25H23N9O6S

References

– [1]Juif PE, et al. Clinical Pharmacology of Clazosentan, a Selective Endothelin A Receptor Antagonist for the Prevention and Treatment of aSAH-Related Cerebral Vasospasm. Front Pharmacol. 2021 Feb 4;11:628956. |[2]Povlsen GK, et al. MEK1/2 inhibitor U0126 but not endothelin receptor antagonist clazosentan reduces upregulation of cerebrovascular contractile receptors and delayed cerebral ischemia, and improves outcome after subarachnoid hemorrhage in rats. J Cereb Blood Flow Metab. 2015 Feb;35(2):329-37. |[3]Vatter H, et al. Cerebrovascular characterization of clazosentan, the first nonpeptide endothelin receptor antagonist clinically effective for the treatment of cerebral vasospasm. Part I: inhibitory effect on endothelin(A) receptor-mediated contraction. J Neurosurg. 2005 Jun;102(6):1101-7. |[4]Verri WA Jr, Guerrero AT, Fukada SY, Valerio DA, Cunha TM, Xu D, Ferreira SH, Liew FY, Cunha FQ. IL-33 mediates antigen-induced cutaneous and articular hypernociception in mice. Proc Natl Acad Sci U S A. 2008 Feb 19;105(7):2723-8. |[5]Juif PE, et al. Influence of Rifampin-Mediated Organic Anion-Transporting Polypeptide 1B1/1B3 Inhibition on the Pharmacokinetics of Clazosentan. Clin Transl Sci. 2019 Sep;12(5):440-444.

CAS Number

– 180384-56-9

Molecular Weight

– 577.57

Compound Purity

– 98.01

SMILES

– O=S(C1=NC=C(C)C=C1)(NC2=NC(C3=CC(C4=NNN=N4)=NC=C3)=NC(OCCO)=C2OC5=CC=CC=C5OC)=O

Clinical Information

– Phase 3

Research Area

– Cardiovascular Disease

Solubility

– DMSO : 83.33 mg/mL (ultrasonic)

Target

– Endothelin Receptor

Pathway

– GPCR/G Protein

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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