Sitaxsentan-13C6
Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan (HY-76520). 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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C1213C6H13ClN2O6S2
- Masse moléculaire:458.84
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
ETA 1.4 nM (IC50) |
ETA 0.43 nM (Ki) |
ETB 9800 nM (IC50) |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
-
Unlabeled Cas 184036-34-8
-
Masse moléculaire 458.84
-
Formule C1213C6H13ClN2O6S2
-
SMILES
O=S(C1=C(C(C[13C]2=[13C][13C]3=[13C]([13C]=[13C]2C)OCO3)=O)SC=C1)(NC4=C(C(C)=NO4)Cl)=O
-
Synonyms
IPI 1040-13C6 ; TBC-11251-13C6
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Rondelet B, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension. Am J Physiol Heart Circ Physiol. 2010 Oct;299(4):H1118-23. Epub 2010 Aug 6. [Content Brief]
[2]. Tilton RG, et al. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist. Pulm Pharmacol Ther. 2000;13(2):87-97. [Content Brief]
[3]. Hartman JC, et al. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol. 2010 Jun;88 [Content Brief]
[4]. Wu C, et al. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem. 1997 May 23;40(11):1690-7. [Content Brief]
[5]. Lepist EI, et al. Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes. PLoS One. 2014 Jan 30;9(1):e87548. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sitaxsentan-13C6 Related Classifications
HY-76520S Related Classifications
Powered by Bioz