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Sitaxsentan sodium

Cat. No. M2029
Sitaxsentan sodium Structure
Synonym:

TBC-11251

Size Price Availability Quantity
10mg USD 150  USD150 In stock
50mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

Sitaxsentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki value of 1.4 nM and 0.43 nM, respectively. Sitaxsentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0. Sitaxsentan blocks the action of endothelin (ET) on the endothelin-A (ETA) receptor selectively (by a factor of 6000 compared to the ETB). Sitaxsentan blocked increased plasma endothelin levels in the prevention protocol but did not affect the established elevated levels in the intervention study.

Chemical Information
Molecular Weight 476.89
Formula C18H14ClN2NaO6S2
CAS Number 210421-74-2
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Girgis RE, et al. Ann Rheum Dis. Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease.

[2] Langleben D, et al. J Cardiovasc Pharmacol. STRIDE 1: effects of the selective ET(A) receptor antagonist, sitaxsentan sodium, in a patient population with pulmonary arterial hypertension that meets traditional inclusion criteria of previous pulmonary arterial hypertension trials.

[3] Tilton RG, et al. Pulm Pharmacol Ther. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist.

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Keywords: Sitaxsentan sodium, TBC-11251 supplier, Endothelin Receptor, inhibitors, activators


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