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Sitaxsentan sodium

Cat. No. M2029

Sitaxsentan sodium Structure

Synonym: TBC-11251

Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 795 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 476.89
Formula C18H14ClN2NaO6S2
CAS Number 210421-74-2
Purity >99%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease.
Girgis RE, et al. Ann Rheum Dis. 2007 Nov;66(11):1467-72. PMID: 17472992.

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.
Langleben D, et al. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S80-4. PMID: 15838366.

Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist.
Tilton RG, et al. Pulm Pharmacol Ther. 2000;13(2):87-97. PMID: 10799286.

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

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