Sitaxsentan-sodium-IPI-1040-sodium-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESitaxsentan sodiumCat. No.: HY-11103CAS No.: 210421-74-2Synonyms: IPI 1040 (sodium); TBC11251 (sodium)分式: CHClNNaOS分量: 476.89作靶点: Endothelin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-2

2、0C 1 month溶解性数据体外实验 DMSO : 107 mg/mL (224.37 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0969 mL 10.4846 mL 20.9692 mL5 mM 0.4194 mL 2.0969 mL 4.1938 mL10 mM 0.2097 mL 1.0485 mL 2.0969 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVI

3、TY物活性 Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium)种有效的，选择性的 endothelin A receptor 拮抗剂。体外研究Sitaxsentan and Bosentan attenuate NTCP transport at higher concentrations, and inhibit human hepatictransporters, which provides a potential mechanism for the increased hepatotoxicity observed for the

4、se1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEagents in the clinical setting. Only sitaxsentan decreased OATP transport (52%) 1. Sitaxsentan andsitaxsentan combined with sildenafil completely prevent the increased expressions of endothelin-1 and of theETB receptor. Sitaxsentan alone partially r

5、estores the expressions of BMPR-1A and BMPR-2. Thecombination of sildenafil and sitaxsentan further restores the expressions of BMPR-1A and BMPR-2, whichremaines, however, decreased compared with controls 3.体内研究 Sitaxsentan (5 mg/kg infused iv 10 min prior to onset of hypoxia) completely blocks hypo

6、xia-inducedvasoconstriction 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 tonormal oxygen levels is without effect on MPAP 2. Sitaxsentan alone limits shunt-i

7、nduced increase in MT.Sitaxsentan combined with sildenafil more effectively prevents this remodeling, which, however, tends toremain increased compared with controls 3.PROTOCOLAnimal After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30 mg/kg body weight per dayAdministra

8、tion 2 in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia. At the conclusionof 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 m

9、ethods. They are for reference only.REFERENCES1. Hartman JC, et al. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substratesand inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol. 2010 Jun

10、;882. 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):87-97.3. Rondelet B, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension. Am J Physiol Heart CircPhysiol. 2010 Oct;299(4):H1118-23. Epub 2010 Aug 6.McePdfHeightCaution: Product has not been fully