Merck
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PZ0203

Sigma-Aldrich

Sitaxentan sodium salt

≥98% (HPLC)

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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
PubChem Substance ID:
329823772
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Pfizer®

color

white to beige

solubility

H2O: 10 mg/mL (clear solution)

originator

Pfizer

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)

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Sitaxentan sodium salt ≥98% (HPLC)

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Sigma-Aldrich

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Danshensu sodium salt ≥98% (HPLC)

Sigma-Aldrich

SML0679

Danshensu sodium salt

form

powder

form

powder

form

powder

form

powder

manufacturer/tradename

Pfizer®

manufacturer/tradename

-

manufacturer/tradename

-

manufacturer/tradename

-

color

white to beige

color

-

color

white to beige

color

white to beige

solubility

H2O: 10 mg/mL (clear solution)

solubility

water: 50 mg/mL, clear, colorless

solubility

H2O: 10 mg/mL, clear

solubility

H2O: 20 mg/mL, clear

originator

Pfizer

originator

-

originator

-

originator

-

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).

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.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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