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Etavopivat

Chemical Structure : Etavopivat

CAS No.: 2245053-57-8

Etavopivat (FT-4202)

Catalog No.: PC-72959Not For Human Use, Lab Use Only.

Etavopivat (FT-4202) is a novel oral activator of PKR that decreases 2,3-DPG levels and hence would increase the HbS O2 affinity to reduce sickling.

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Biological Activity

Etavopivat (FT-4202) is a novel oral activator of PKR that decreases 2,3-DPG levels and hence would increase the HbS O2 affinity to reduce sickling.
FT-4202 increases the hemoglobin S O2 affinity to reduce sickling and improve RBC membrane deformability.
Etavopivat (FT-4202) increased Hb-oxygen affinity and reduced sickling under deoxygenation in ex vivo RBCs from donors with sickle cell disease (SCD).
Oral administration of FT-4202 increases Hb and improves RBC parameters in BERK mice.
Etavopivat is currently being evaluated in clinical trials for the treatment sickle cell disease (SCD).

Physicochemical Properties

M.Wt 457.501
Formula C22H23N3O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-1-(5-(2,3-Dihydro(1,4)dioxino(2,3-b)pyridine-7- sulfonyl)-3,4,5,6-tetrahydropyrrolo(3,4-C)pyrrol-2(1H)- YL)-3-hydroxy-2-phenylpropan-1-one

References

1. Shrestha A, et al. Blood Adv. 2021 May 11;5(9):2385-2390.

2. Forsyth S, et al. Clin Pharmacol Drug Dev. 2022 Jan 12.

3. Schroeder P, et al. J Pharmacol Exp Ther. 2022 Mar;380(3):210-219.

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