Voxelotor_product_DataBase

Bioactivity	Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment[1].
Target	HbS polymerization
Invitro	Voxelotor (GBT440) binds to the N-terminal a chain of haemoglobin (Hb), increases haemoglobin S (HbS) affinity for oxygen, delays in vitro HbS polymerization and prevents sickling of red blood cells (RBCs)[1].
In Vivo	Voxelotor (GBT440; 100-150 mg/kg; administered twice a day by oral gavage for 9-12 days) reduces ex vivo sickling and prolongs red blood cells (RBCs) half-life in a murine model of sickle cell disease (SCD)[1].Voxelotor shows T1/2s of 11.7, 19.1±1.5, 66.0±11, 28.8±4.0 hours for mouse (70 mg/kg; i.v.), rat (1.6 mg/kg; i.v.), dog (1 mg/kg; i.v.), and momkey (1 mg/kg; i.v.), respectively[1].Voxelotor shows Cmaxs of 81.9, 71.2±6.0, 5.56±1.6, and 25.2±5.5 μg/mL for mouse (30 mg/kg; p.o.), rat (7.2 mg/kg; p.o.), dog (2.5 mg/kg; p.o.), and momkey (4.25 mg/kg; p.o.), respectively[1]. Animal Model:
Name	Voxelotor
CAS	1446321-46-5
Formula	C19H19N3O3
Molar Mass	337.37
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Reference	[1]. Oksenberg D, et al. GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell disease. Br J Haematol. 2016 Oct;175(1):141-53. [2]. Metcalf B, Chuang C, Dufu K, et al. Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. ACS Med Chem Lett. 2017;8(3):321-326.

PeptideDB

Voxelotor

CAS: 1446321-46-5 F: C19H19N3O3 W: 337.37