Etavopivat
Based on 1 Customer Validation
Etavopivat is a potent, selective, and orally active erythrocyte pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects that can be used in studies of sickle cell disease and other haemoglobinopathies.
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- Pureté: 99.91%
- CAS No.: 2245053-57-8
- Formule: C22H23N3O6S
- Masse moléculaire:457.50
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Etavopivat (20 μM, 4 h) improves haemoglobin-oxygen affinity and reduces the sickle point (PoS) in human red blood cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Etavopivat (3-22 mg/kg, p.o., daily, 5 days) causes an increase in 2,3-DPG and ATP in crab-eating monkeys at doses of 8 mg/kg and 22 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCA mice[1]
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Dosage:500-1000 mg/kg
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Administration:p.o., daily, 2 weeks
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Result:Decreased the levels of 2,3-DPG.
Increased ATP levels.
Reduced sickling in vivo.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2245053-57-8
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Appearance Solid
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Masse moléculaire 457.50
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Formule C22H23N3O6S
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Color White to off-white
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SMILES
O=S(N1CC2=C(CN(C2)C([C@@H](C3=CC=CC=C3)CO)=O)C1)(C4=CN=C(OCCO5)C5=C4)=O
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Synonyms
FT-4202
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (109.29 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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Shrestha A, et al. FT-4202, an oral PKR activator, has potent antisickling effects and improves RBC survival and Hb levels in SCA mice. Blood Adv. 2021 May 11;5(9):2385-2390. [Content Brief]
[2]. Schroeder P, et al. Etavopivat, a Pyruvate Kinase Activator in Red Blood Cells, for the Treatment of Sickle Cell Disease. J Pharmacol Exp Ther. 2022 Mar;380(3):210-219. [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 |
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| DMSO | 1 mM | 2.1858 mL | 10.9290 mL | 21.8579 mL | 54.6448 mL |
| 5 mM | 0.4372 mL | 2.1858 mL | 4.3716 mL | 10.9290 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1858 mL | 5.4645 mL | |
| 15 mM | 0.1457 mL | 0.7286 mL | 1.4572 mL | 3.6430 mL | |
| 20 mM | 0.1093 mL | 0.5464 mL | 1.0929 mL | 2.7322 mL | |
| 25 mM | 0.0874 mL | 0.4372 mL | 0.8743 mL | 2.1858 mL | |
| 30 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8215 mL | |
| 40 mM | 0.0546 mL | 0.2732 mL | 0.5464 mL | 1.3661 mL | |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL | 1.0929 mL | |
| 60 mM | 0.0364 mL | 0.1821 mL | 0.3643 mL | 0.9107 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6831 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5464 mL |
Etavopivat Related Classifications
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