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Sitaxsentan sodium

Catalog No. T6672   CAS 210421-74-2
Synonyms: TBC11251 sodium salt, TBC11251, Thelin, Sitaxentan sodium

Sitaxsentan sodium (TBC11251 sodium salt) is a highly selective antagonist of endothelin A receptors.

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Sitaxsentan sodium Chemical Structure
Sitaxsentan sodium, CAS 210421-74-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 97.00
25 mg In stock $ 173.00
50 mg In stock $ 328.00
100 mg In stock $ 563.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 99%
Purity: 98.39%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sitaxsentan sodium (TBC11251 sodium salt) is a highly selective antagonist of endothelin A receptors.
Targets&IC50 ETA:1.4 nM
Kinase Assay Ligand binding studies: Binding studies are performed in a 30 mM HEPES buffer, pH 7.4, containing 150 mM NaCl, 5 mM MgCl2, and 0.05% bacitracin using 2 mg/tube (ETA) or 0.75 mg/tube (ETB) membrane. Sitaxentan sodium is dissolved in DMSO and diluted with the assay buffer to give a final concentration of 0.25% DMSO. Competitive inhibition experiments are performed in triplicate in a final volume of 200 μL containing 4 pM [125I]ET-1 (1.6 nCi). Nonspecific binding is determined in the presence of 100 nM ET-1. Samples are incubated for 16 hours?18 hours at 24 °C. One milliliter of PBS is then added and the assay centrifuged at 2000 g for 25 minutes at 4 °C. The supernatant is decanted and the membrane bound radioactivity counted on a Genesys gamma counter.
Cell Research TE 671 or transfected COS 7 cells are grown to confluence in six-well plates. Sixteen hours prior to use, the media in each well is replaced with 2 mL of inositol-free RPMI-164 (IF-RPMI) media containing 10% inositol-free FCS and 2 mCi [3H]myoinositol and incubated at 37 °C in the presence of 6% CO2. The media is aspirated, and the cells are washed twice with PBS. Cells are preincubated for 10 minutes in 1 mL of lithium buffer (15 μM HEPES, pH 7.4, 145 μM NaCl, 5.4 μM KCl, 1.8 μM CaCl2, 0.8 μM MgSO4, 1.0 μM NaH2PO4, 11.2 μM glucose, 20 μM LiCl) with or without Sitaxentan sodium prior to the addition of 100 μM of ET-1 at different concentrations. Cells are then incubated for an additional 45 minutes. The buffer is discarded, and the accumulated inositol phosphates are extracted with ice cold methanol. The total cell protein in each well is measured using the BCA assay after solubilizing the cells in 0.1 M NaOH.(Only for Reference)
Animal Research Sitaxsentan is formulated in water.After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30 mg/kg body weight per day in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia. At the conclusion of the 4 week period of hypoxia, femoral and pulmonary arterial cannulation and measurement of MPAP, MSAP, and HR are performed.
Synonyms TBC11251 sodium salt, TBC11251, Thelin, Sitaxentan sodium
Molecular Weight 476.89
Formula C18H14ClN2O6S2·Na
CAS No. 210421-74-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40 mg/mL (83.87 mM)

Ethanol: 20 mg/mL (41.93 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Wu C, et al. J Med Chem. 1997, 40(11), 1690-1697. 2. Tilton RG, et al. Pulm Pharmacol Ther. 2000, 13(2), 87-97. 3. Wanebo JE, et al. Neurosurgery. 1998, 43(6), 1409-1417. 4. Holm P. Scand Cardiovasc J Suppl. 1997, 46, 1-40.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Orally Active Compound Library Pediatric Drug Library Bioactive Compounds Library Max GPCR Compound Library Anti-Cardiovascular Disease Compound Library ReFRAME Related Library Inhibitor Library Neurotransmitter Receptor Compound Library Bioactive Compound Library

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Keywords

Sitaxsentan sodium 210421-74-2 GPCR/G Protein Endothelin Receptor IPI1040 TBC-11251 Inhibitor IPI-1040 TBC11251 sodium salt Sitaxsentan inhibit TBC 11251 TBC11251 sodium TBC11251 IPI 1040 Thelin Sitaxentan sodium inhibitor

 

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