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Sitaxsentan
CAS No. 184036-34-8
Sitaxsentan( IPI-1040 | Sitaxentan | TBC-11251 )
Catalog No. M12843 CAS No. 184036-34-8
A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 190 | Get Quote |
|
| 10MG | 311 | Get Quote |
|
| 25MG | 483 | Get Quote |
|
| 50MG | 654 | Get Quote |
|
| 100MG | 888 | Get Quote |
|
| 500MG | 1782 | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameSitaxsentan
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
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DescriptionA potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM; dispalys >5,000-fold selectivity over ETB receptors; inhibits ET1-induced stimulation of phosphoinositide turnover with Ki of 0.686 nM, and pA2 of 8.0; excellent PK profile and oral bioavailability.Hypertension Withdrawn.
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In Vitro——
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In Vivo——
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SynonymsIPI-1040 | Sitaxentan | TBC-11251
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PathwayGPCR/G Protein
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TargetEndothelin Receptor
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RecptorEndothelin Receptor
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Research AreaCardiovascular Disease
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IndicationHypertension
Chemical Information
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CAS Number184036-34-8
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Formula Weight454.9045
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Molecular FormulaC18H15ClN2O6S2
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCC1=CC2=C(C=C1CC(=O)C3=C(C=CS3)S(=O)(=O)NC4=C(C(=NO4)C)Cl)OCO2
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Chemical Name3-Thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Wu C, et al. J Med Chem. 1997 May 23;40(11):1690-7.
2. Wanebo JE, et al. Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8.
3. Tilton RG, et al. Pulm Pharmacol Ther. 2000;13(2):87-97.
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