Fandosentan potassium
Fandosentan potassium is a potent endothelin A receptor (ETAR) antagonist. Fandosentan potassium inhibits CYP2C9 and CYP3A4 activities with IC50 values of 39.6 and 21.6 μM, respectively. Fandosentan potassium reverses the hypoxic pulmonary vasoconstriction in the perinatal lamb. Fandosentan potassium can be used for pulmonary hypertension research[1][2].
For research use only. We do not sell to patients.
- CAS No.: 221246-12-4
- Formula: C25H17F3KNO6S
- Molecular Weight:555.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
CYP3A4 21.6 μM (IC50) |
CYP2C9 39.6 μM (IC50) |
Chemical Information
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CAS No. 221246-12-4
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Molecular Weight 555.56
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Formula C25H17F3KNO6S
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SMILES
O=C(C(N1C2=C(C=CC=C2)C(F)(F)F)=C(C3=CC4=C(OCO4)C(CC)=C3)C5=CC=CC=C5S1(=O)=O)O[K]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
References
[1]. Sahi J, et al. Metabolism and transporter-mediated drug-drug interactions of the endothelin-A receptor antagonist CI-1034. Chem Biol Interact. 2006 Feb 1;159(2):156-68. [Content Brief]
[2]. Coe Y, et al. The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in the perinatal lamb. J Pharmacol Exp Ther. 2002 Aug;302(2):672-80. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)