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
Quality Level
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
Sitaxentan is a potent and selective endothelin ET(A) receptor antagonist; antihypertensive.
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).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Sitaxsentan for the prevention of experimental shunt-induced pulmonary hypertension
Rondelet B, et al.
Pediatric Research, 61(3), 284-284 (2007)
Alex G Cuenca et al.
Innate immunity, 21(4), 386-391 (2014-08-12)
Neonates have increased susceptibility to infection, which leads to increased mortality. Whether or not this as a result of implicit deficits in neonatal innate immune function or recapitulation of innate immune effector cell populations following infection is unknown. Here, we
Daan van de Velde et al.
Biomedical chromatography : BMC, 34(3), e4787-e4787 (2019-12-26)
Endothelin receptor antagonists (ERAs) such as, ambrisentan, macitentan and sitaxentan are primarily used for the treatment of pulmonary arterial hypertension. Considering the rise in endothelin in pre-eclampsia, ERAs may also be useful in its treatment. To evaluate the pharmacokinetics of
Global Trade Item Number
| SKU | GTIN |
|---|---|
| PZ0203-5MG | 04061832899251 |
| PZ0203-25MG | 04061832899244 |