1. GPCR/G Protein
  2. Endothelin Receptor
  3. Sitaxsentan sodium

Sitaxsentan sodium (Synonyms: IPI 1040 sodium; TBC11251 sodium)

Cat. No.: HY-11103 Purity: 98.73%
Handling Instructions

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.

For research use only. We do not sell to patients.

Sitaxsentan sodium Chemical Structure

Sitaxsentan sodium Chemical Structure

CAS No. : 210421-74-2

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Description

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.

In Vitro

Sitaxsentan and Bosentan attenuate NTCP transport at higher concentrations, and inhibit human hepatic transporters, which provides a potential mechanism for the increased hepatotoxicity observed for these agents in the clinical setting. Only sitaxsentan decreased OATP transport (52%)[1]. Sitaxsentan and sitaxsentan combined with sildenafil completely prevent the increased expressions of endothelin-1 and of the ETB receptor. Sitaxsentan alone partially restores the expressions of BMPR-1A and BMPR-2. The combination of sildenafil and sitaxsentan further restores the expressions of BMPR-1A and BMPR-2, which remaines, however, decreased compared with controls[3].

In Vivo

Sitaxsentan (5 mg/kg infused iv 10 min prior to onset of hypoxia) completely blocks hypoxia-induced vasoconstriction and this group does not differ from air controls. Oral administration of sitaxsentan, significantly attenuates the increase in MPAP, while the administration of sitaxsentan to rats exposed to normal oxygen levels is without effect on MPAP[2]. Sitaxsentan alone limits shunt-induced increase in MT. Sitaxsentan combined with sildenafil more effectively prevents this remodeling, which, however, tends to remain increased compared with controls[3].

Clinical Trial
Molecular Weight

476.89

Formula

C₁₈H₁₄ClN₂NaO₆S₂

CAS No.

210421-74-2

SMILES

O=S(C1=C(SC=C1)C(CC2=C(C=C3OCOC3=C2)C)=O)(N([Na])C4=C(C(C)=NO4)Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0969 mL 10.4846 mL 20.9692 mL
5 mM 0.4194 mL 2.0969 mL 4.1938 mL
10 mM 0.2097 mL 1.0485 mL 2.0969 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30 mg/kg body weight per day in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia. At the conclusion of the 4 week period of hypoxia, femoral and pulmonary arterial cannulation and measurement of MPAP, MSAP, and HR are performed.

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

References

Purity: 98.73%

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Keywords:

SitaxsentanIPI 1040TBC11251IPI1040IPI-1040TBC 11251TBC-11251Endothelin ReceptorInhibitorinhibitorinhibit

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Product Name:
Sitaxsentan sodium
Cat. No.:
HY-11103
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