Clazosentan
Based on 1 publication(s) in Google Scholar
Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction.
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- Pureté: 99.50%
- CAS No.: 180384-56-9
- Formule: C25H23N9O6S
- Masse moléculaire:577.57
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Clazosentan
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.7 nM
Compound: 24
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Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
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[PMID: 27321813] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[2]
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Dosage:10 μM, 0.05 mL/kg
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Administration:Intracisternal injection
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Result:Inhibited the contractile responses to ET-1, without preventing SAH-induced upregulation of ET receptors in cerebral arteries.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 180384-56-9
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Appearance Solid
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Masse moléculaire 577.57
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Formule C25H23N9O6S
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Color Off-white to light yellow
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SMILES
O=S(C1=NC=C(C)C=C1)(NC2=NC(C3=CC(C4=NNN=N4)=NC=C3)=NC(OCCO)=C2OC5=CC=CC=C5OC)=O
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Synonyms
Ro 61-1790; VML 588; AXV-034343
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 83.33 mg/mL (144.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Juif PE, et al. Clinical Pharmacology of Clazosentan, a Selective Endothelin A Receptor Antagonist for the Prevention and Treatment of aSAH-Related Cerebral Vasospasm. Front Pharmacol. 2021 Feb 4;11:628956. [Content Brief]
[2]. Povlsen GK, et al. MEK1/2 inhibitor U0126 but not endothelin receptor antagonist clazosentan reduces upregulation of cerebrovascular contractile receptors and delayed cerebral ischemia, and improves outcome after subarachnoid hemorrhage in rats. J Cereb Blood Flow Metab. 2015 Feb;35(2):329-37. [Content Brief]
[3]. Vatter H, et al. Cerebrovascular characterization of clazosentan, the first nonpeptide endothelin receptor antagonist clinically effective for the treatment of cerebral vasospasm. Part I: inhibitory effect on endothelin(A) receptor-mediated contraction. J Neurosurg. 2005 Jun;102(6):1101-7. [Content Brief]
[4]. Verri WA Jr, Guerrero AT, Fukada SY, Valerio DA, Cunha TM, Xu D, Ferreira SH, Liew FY, Cunha FQ. IL-33 mediates antigen-induced cutaneous and articular hypernociception in mice. Proc Natl Acad Sci U S A. 2008 Feb 19;105(7):2723-8. [Content Brief]
[5]. Juif PE, et al. Influence of Rifampin-Mediated Organic Anion-Transporting Polypeptide 1B1/1B3 Inhibition on the Pharmacokinetics of Clazosentan. Clin Transl Sci. 2019 Sep;12(5):440-444. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7314 mL | 8.6570 mL | 17.3139 mL | 43.2848 mL |
| 5 mM | 0.3463 mL | 1.7314 mL | 3.4628 mL | 8.6570 mL | |
| 10 mM | 0.1731 mL | 0.8657 mL | 1.7314 mL | 4.3285 mL | |
| 15 mM | 0.1154 mL | 0.5771 mL | 1.1543 mL | 2.8857 mL | |
| 20 mM | 0.0866 mL | 0.4328 mL | 0.8657 mL | 2.1642 mL | |
| 25 mM | 0.0693 mL | 0.3463 mL | 0.6926 mL | 1.7314 mL | |
| 30 mM | 0.0577 mL | 0.2886 mL | 0.5771 mL | 1.4428 mL | |
| 40 mM | 0.0433 mL | 0.2164 mL | 0.4328 mL | 1.0821 mL | |
| 50 mM | 0.0346 mL | 0.1731 mL | 0.3463 mL | 0.8657 mL | |
| 60 mM | 0.0289 mL | 0.1443 mL | 0.2886 mL | 0.7214 mL | |
| 80 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5411 mL | |
| 100 mM | 0.0173 mL | 0.0866 mL | 0.1731 mL | 0.4328 mL |
Clazosentan Related Classifications
HY-17352 Related Classifications
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