Sitaxentan sodium salt, >=98% (HPLC)

Biochem/physiol Actions

Sitaxentan (Sitaxsentan) is a potent and selective endothelin ET(A) receptor antagonist once used in the treatment of pulmonary arterial hypertension (PAH), but removed from the market because of hepatotoxicity. It is over 6000-fold selective for the the ETA receptor subtype with an IC₅₀ of 1 nM for ETA versus an IC₅₀ of 9800 nM for ETB.

Sitaxsentan prevents shunt mediated elevation of pulmonary vascular resistance (PVR). Sitaxsentan effectively inhibits basolateral Na⁺-taurocholate cotransporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and bile salt export pump (BSEP).

Legal Information

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Sold for research purposes under agreement from Pfizer Inc.

Other Notes

This compound was developed by Pfizer for Neuroscience research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Packaging

5, 25 mg in glass bottle