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210421-74-2 (Sitaxsentan (sodium))

1

Identification

Sitaxsentan (sodium) Sitaxsentan (sodium)
Name Sitaxsentan (sodium)
Formula C18H14ClN2NaO6S2
MW 476.89
CAS No. 210421-74-2
EINECS
Smiles O=S([N-]C1=C(C(C)=NO1)Cl)(C2=C(SC=C2)C(CC3=C(C=C4OCOC4=C3)C)=O)=O.[Na+]
Synonyms THELIN ; TBC11251 sodium salt; TBC11251; sodium (4-chloro-3-methylisoxazol-5-yl)((2-(2-(6-methylbenzo[d][1,3]dioxol-5-yl)acetyl)thiophen-3-yl)sulfonyl)amide
InChI InChI=1S/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1
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Introduction

Sitaxsentan sodium (IPI 1040; TBC 11251) is a selective endothelin A (ETA) receptor antagonist.

Background Information

A selective endothelin A (ETA) receptor antagonist ......by AOBIOUS INC
Sitaxsentan sodium (IPI 1040; TBC 11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. IC50 value: Target: ETA receptor ......by MedChemexpress Co., Ltd.
Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3. ......by Selleck Chemicals LLC
Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Cell lines TE 671 or transfected COS 7 cells
Conditions 0 μM -10 μM; 45 minutes
Method 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.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Adult Sprague−Dawley rats and male beagle dogs
Dosage 50 mg/kg
Formulation
Administration i.v., p.o.
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:Light yellow to yellow solid EBNumber:EB000028802

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 40 mg/mL (83.87 mM); Ethanol20 mg/mL (41.93 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Sitaxsentan (sodium) - Withdrawn
Sitaxsentan (sodium) Pfizer Inc Pulmonary hypertension 2009/12/31 2011/3/31 Phase 4 Clinical
Sitaxsentan (sodium) Pfizer Japan Inc Pulmonary artery hypertension 2010/11/30 2010/12/1 Phase 3 Clinical
Sitaxsentan (sodium) Pfizer Inc Pulmonary artery hypertension 2010/8/31 2010/11/1 Phase 3 Clinical
Sitaxsentan (sodium) Pfizer Inc Pulmonary hypertension 2003/3/31 2011/7/1 Phase 3 Clinical
Sitaxsentan (sodium) Pfizer Inc Pulmonary hypertension 2009/5/31 2011/4/1 Phase 3 Clinical
Sitaxsentan (sodium) - No Development Reported
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Safety Data of Sitaxsentan (sodium)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD15() USA
CHEMSCENE, LLC 50mg/USD680(In stock);100mg/USD950(In stock) USA
MedChemexpress Co., Ltd. 10mg/USD200(In stock);50mg/USD680(In stock);100mg/USD950(In stock) USA
Melone Pharmaceutical Co., Ltd. China
Selleck Chemicals LLC 5mg/USD210(In stock);10mg/USD270(In stock);10mM/1mLIn DMSO/USD400(In stock);50mg/USD970(In stock);100mg/USD1270(In stock) USA
Shanghai DND Pharm-Technology Co., Inc. China
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD200(In stock);50mg/USD680(In stock);100mg/USD950(In stock) China
Target Molecule Corp. 10mg/USD152();100mg/USD488() USA
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Related Products

Other Forms of 210421-74-2

Name CAS No Formula MW
Sitaxsentan (phosphate (1:1) salt) 215501-46-5 C18H17ClN2O10PS2- 551.89
sitaxsentan 184036-34-8 C18H15ClN2O6S2 454.9

Recommended Compounds in Endothelin Receptor

Name CAS No Formula MW
ACT-132577 1103522-45-7 C16H14Br2N6O4S 546.19
BQ-788 (sodium salt) 156161-89-6 C34H50N5NaO7 663.78
Sulfisoxazole 127-69-5 C11H13N3O3S 267.3
Atrasentan (hydrochloride) 195733-43-8 C29H39ClN2O6 547.08
Bosentan (hydrate) 157212-55-0 C27H31N5O7S 569.63
SPI-1620 142569-99-1 C83H112N19O25 1775.89
Atrasentan 173937-91-2 C29H38N2O6 510.62
Sitaxsentan (phosphate (1:1) salt) 215501-46-5 C18H17ClN2O10PS2- 551.89
Macitentan 441798-33-0 C19H20Br2N6O4S 588.27
Avosentan 290815-26-8 C23H21N5O5S 479.51
Zibotentan 186497-07-4 C19H16N6O4S 424.43
Ambrisentan 177036-94-1 C22H22N2O4 378.42
sitaxsentan 184036-34-8 C18H15ClN2O6S2 454.9
Bosentan 147536-97-8 C27H29N5O6S 551.61
Endothelin 1 117399-94-7 C109H159N25O32S5 2491.9
Cyclo(D-alpha-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl) 136553-81-6 C31H42N6O7 610.7
Aminaftone 14748-94-8 C18H15NO4 309.32
Ro 46-2005 150725-87-4 C23H27N3O6S 473.54
ZD-1611 186497-38-1 C22H24N4O5S 456.51
Macitentan (n-butyl analogue) 556797-16-1 C20H21Br2N5O4S 587.28

Recommended Compounds in Same Indication

Name CAS No Formula MW
sitaxsentan 184036-34-8 C18H15ClN2O6S2 454.9
Tadalafil 171596-29-5 C22H19N3O4 389.4
Sildenafil (citrate) 171599-83-0 C28H38N6O11S 666.7
Milrinone 78415-72-2 C12H9N3O 211.22
Macitentan 441798-33-0 C19H20Br2N6O4S 588.27
Riociguat 625115-55-1 C20H19FN8O2 422.42
Sildenafil 139755-83-2 C22H30N6O4S 474.58
Bosentan 147536-97-8 C27H29N5O6S 551.61
Ambrisentan 177036-94-1 C22H22N2O4 378.42
Cleviprex 167221-71-8 C21H23Cl2NO6 456.32
Bosentan (hydrate) 157212-55-0 C27H31N5O7S 569.63
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Route of Synthesis

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References

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More Information

Sitaxsentan (sodium)

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