PZ0203

Sitaxentan sodium salt

≥98% (HPLC)

• Synonym(s): N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide sodium salt, Sitaxsentan sodium salt, TBC-11251 sodium salt, Thelin
• Empirical Formula (Hill Notation): C₁₈H₁₄ClN₂NaO₆S₂
• CAS Number: 210421-74-2
• Molecular Weight: 476.89
• UNSPSC Code: 51111800
• PubChem Substance ID: 329823772
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: H₂O: 10 mg/mL (clear solution)
• storage temp.: room temp
• SMILES string: [Na+].Cc1cc2OCOc2cc1CC(=O)c3sccc3S(=O)(=O)[N-]c4onc(C)c4Cl
• InChI: 1S/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1
• InChI key: MDTNUYUCUYPIHE-UHFFFAOYSA-N
• Gene Information: human ... EDNRA(1909) , EDNRB(1910)

Description

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).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable