| Identification | Back Directory | [Name]
1-Propanone, 1-[5-[(2,3-dihydro-1,4-dioxino[2,3-b]pyridin-7-yl)sulfonyl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]-3-hydroxy-2-phenyl-, (2S)- | [CAS]
2245053-57-8 | [Synonyms]
FT-4202
Etavopivat
1-Propanone, 1-[5-[(2,3-dihydro-1,4-dioxino[2,3-b]pyridin-7-yl)sulfonyl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]-3-hydroxy-2-phenyl-, (2S)- | [Molecular Formula]
C22H23N3O6S | [MOL File]
2245053-57-8.mol | [Molecular Weight]
457.5 |
| Chemical Properties | Back Directory | [Boiling point ]
725.2±70.0 °C(Predicted) | [density ]
1.53±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
14.27±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
Etavopivat (500-1000 mg/kg, p.o., daily, 2 weeks) improves RBC survival and Hb levels in SCA mice[1].
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].
| Animal Model: | SCA mice[1] | | Dosage: | 500-1000 mg/kg | | Administration: | p.o., daily, 2 weeks | | Result: | Decreased the levels of 2,3-DPG.
Increased ATP levels.
Reduced sickling in vivo.
|
| [storage]
Store at -20°C | [References]
[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. DOI:10.1182/bloodadvances.2020003604
[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. DOI:10.1124/jpet.121.000743 |
|
|