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
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About This Item
Empirical Formula (Hill Notation):
C18H14ClN2NaO6S2
CAS Number:
Molecular Weight:
476.89
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
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)
Biochem/physiol Actions
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).
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.
Sitaxentan is a potent and selective endothelin ET(A) receptor antagonist; antihypertensive.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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