OXBRYTA
Voxelotor
CAS: 1446321-46-5
Molecular Formula: C19H19N3O3
OXBRYTA - Names and Identifiers
OXBRYTA - Physico-chemical Properties
| Molecular Formula | C19H19N3O3 |
| Molar Mass | 337.3725 |
| Density | 1.23±0.1 g/cm3(Predicted) |
| Boling Point | 539.2±50.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 7.67±0.10(Predicted) |
| Storage Condition | -20℃ |
OXBRYTA - Upstream Downstream Industry
OXBRYTA - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.964 ml | 14.82 ml | 29.641 ml |
| 5 mM | 0.593 ml | 2.964 ml | 5.928 ml |
| 10 mM | 0.296 ml | 1.482 ml | 2.964 ml |
| 5 mM | 0.059 ml | 0.296 ml | 0.593 ml |
Last Update：2024-01-02 23:10:35
OXBRYTA - Uses and synthesis methods
biological activity
Voxelotor (GBT440, GTx011) is a new type of small molecule compound, which can increase the affinity of hemoglobin and oxygen, and is a hemoglobin regulator.
in vitro study
GBT440 is a new and effective heterotopic effector of sickle-shaped red blood cell hemoglobin, which can improve the affinity of hemoglobin and oxygen, improve its oxygen carrying capacity, and inhibit the formation of polymers in red blood cells under hypoxic conditions. The IC50 of GBT440 to CYP 1A2, 2C8, 2C9, 2C19, 2D6, 3A4 ranges from 7.9 to 148 μM. It is not a substrate for P-gp or BCRP transporters. It can combine with the N-terminal of Hb.
in vivo studies
GBT440 has good oral bioavailability of 60, 37 and 36% respectively in rats, dogs and monkeys. In these several species, there are similar blood and plasma half-lives, about 20 hours. The T 1/2 of GBT440 in all animal species is shorter than that in red blood cells, and the binding of GBT440 to hemoglobin is a reversible process. GBT440 is currently in clinical phase 3 (NCT03036813) in treatment trials for SCD patients. GBT440 can increase the affinity of hemoglobin and oxygen. In a mouse model with sickle cell disease, GBT440 reduces sickle cells and prolongs the half-life of red blood cells. In the SCD mouse model, GBT also prolongs the half-life of red blood cells, reduces the number of reticulocytes, and prevents sickle formation of red blood cells from in vitro. The oral dose suitable for animal models is also suitable for human administration. It can be taken once a day. It is highly selective for red blood cells and has therapeutic safety. Its pharmacokinetics is proportional to the dose, and the terminal half-life is 1.5 to 3 days.
Last Update：2024-04-09 20:52:54
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CAS: 1446321-46-5
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CAS: 1446321-46-5
Tel: 18301782025
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Product Name: GBT 440 Visit Supplier Webpage Request for quotation
CAS: 1446321-46-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1446321-46-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
Raw Materials for OXBRYTA
2-hydroxy-6-(methoxymethoxy)benzaldehyde
3-(chloromethyl)-2-(1-isopropyl-1H-pyrazol-5-yl)pyridine hydrochloride
[2-[1-(propan-2-yl)-1H-pyrazol-5-yl]pyridin-3-yl]methanol
2,6-Dihydroxybenzaldehyde
3-(chloromethyl)-2-(1-isopropyl-1H-pyrazol-5-yl)pyridine hydrochloride
[2-[1-(propan-2-yl)-1H-pyrazol-5-yl]pyridin-3-yl]methanol
2,6-Dihydroxybenzaldehyde