2. GPCR/G Protein TGF-beta/Smad
  3. Endothelin Receptor TGF-β Receptor
  4. Sitaxsentan

Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.

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Sitaxsentan

Sitaxsentan Chemical Structure

CAS No. : 184036-34-8

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Based on 2 publication(s) in Google Scholar

Other Forms of Sitaxsentan:

Sitaxsentan Related Antibodies

Top Publications Citing Use of Products

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ETA ETB

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

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Description

Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension[1][2][3][4][5].

IC50 & Target[4]

ETA

1.4 nM (IC50)

ETA

0.43 nM (Ki)

ETB

9800 nM (IC50)

In Vitro

Sitaxsentan (100 μM, 10 min) significantly inhibits taurocholate cotransporter (NTCP) and organic anion transporter (OATP) transportation in sandwich-cultured human hepatocytes[3].
Sitaxsentan (10 min) has a high efficiency of liver cell uptake and almost no bile excretion[3].
Sitaxsentan has moderate hepatobiliary transporters bile salt export pump (BSEP) inhibition (IC50 = 25 μM) in sandwich-cultured human hepatocytes[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Sitaxsentan Related Antibodies
In Vivo

Sitaxsentan (1.5 mg/kg, p.o., three times a day for 3 months) effectively prevents PAH caused by shunt induction, and the combined medication with Sildenafil (HY-15025) has a better effect in piglets[1].
Sitaxsentan (5 mg/kg, i.v., single dose) completely blocks the activation of ETA receptors in the acute hypoxia model of rats[2].
Sitaxsentan (15-30 mg/kg, p.o., once daily for 2-4 weeks) significantly improves PAH and vascular remodeling caused by chronic hypoxia, but has limited effect on the already formed right ventricular hypertrophy in rat chronic hypoxia model[2].
Sitaxsentan (10-50 mg/kg, p.o., once daily for 3 weeks) dose-dependently improves Monocrotaline(HY-N0750)-induced pulmonary hypertension in rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Shunt-induced PAH model established in piglets (18 days old, 5.3 kg)[1]
Dosage: 1.5 mg/kg or 1.5 mg/kg combined with 0.75 mg/kg Sildenafil
Administration: Oral administration (p.o.) with food, three times a day for 3 months
Result: Combined treatment completely restored the normal state.
Partially inhibited the thickening of blood vessels with single-drug and the combined therapy almost completely prevented it.
Partially restored the expression of BMPR-1A and BMPR-2.
Maintained normal right ventricle-aorta coupling.
Animal Model: Acute hypoxia induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 5 mg/kg
Administration: Intravenous injection (i.v.), 10 minutes before or 50 minutes after the onset of hypoxia
Result: Completely blocked the increase in pressure in prevention group.
Rapidly reversed the elevated MPAP after administration of the drug (reaching normal levels within approximately 30 minutes) in treatment group.
Animal Model: Chronic hypoxia induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 15 mg/kg in prevention group and 15 mg/kg and 30 mg/kg in treatment group
Administration: Oral administration (p.o.) with water, once daily, 48 hours before hypoxia and lasting for 2 weeks or after 2 weeks of hypoxia and lasted for 4 weeks
Result: Decreased The MPAP in the prevention group by 35%, and in the treatment group decreased by 38%.
Reduced the ratio of RV/(LV + S) to some extent.
Improved pulmonary vascular remodeling in both groups.
Animal Model: Monocrotaline induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 10 and 50 mg/kg
Administration: Oral administration (p.o.) with water, once daily for 3 weeks
Result: Improved hemodynamic conditions.
Almost completely prevented pulmonary vascular remodeling at high dose (50mg/kg).
Clinical Trial
Molecular Weight

454.90

Formula

C18H15ClN2O6S2
CAS No.
SMILES

O=S(C1=C(C(CC2=CC3=C(C=C2C)OCO3)=O)SC=C1)(NC4=C(C(C)=NO4)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Sitaxsentan Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sitaxsentan184036-34-8IPI 1040 TBC-11251IPI1040IPI-1040TBC11251TBC 11251TBC-11251Endothelin ReceptorTGF-β ReceptorTransforming growth factor beta receptorsportopulmonary hypertensionbone morphogenetic protein receptor-1Apulmonary arterial hypertensionBMPR-2CYP3A4CYP2C9endothelin A receptorendothelin B receptorsendothelin-1hepatocytesInhibitorinhibitorinhibit

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