Voxelotor
Voxelotor Basic information
- Product Name:
- Voxelotor
- Synonyms:
-
- 2-hydroxy-6-([2-[1-(propan-2-yl)-1H-pyrazol-5-yl]pyridin-3-yl]methoxy)benzaldehyde
- GBT 440
- 2-Hydroxy-6-{[2-(1-isopropyl-1H-pyrazol-5-yl)-3-pyridinyl]methoxy}benzaldehyde
- Hemoglobin Modulators-1
- 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
- Voxelotor(GBT440, GTX011)
- Voxelotor
- Voxelotor, GBT-440, GBT 440, GBT440, GTx-011, GTx011, GTx 011
- CAS:
- 1446321-46-5
- MF:
- C19H19N3O3
- MW:
- 337.37
- Product Categories:
-
- API
- Mol File:
- 1446321-46-5.mol
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Voxelotor Chemical Properties
- Melting point:
- 95 - 97oC
- Boiling point:
- 539.2±50.0 °C(Predicted)
- Density
- 1.23±0.1 g/cm3(Predicted)
- storage temp.
- -20°C Freezer, Under inert atmosphere
- solubility
- Chloroform (Slightly), DMSO (Slightly)
- form
- Solid
- pka
- 7.67±0.10(Predicted)
- color
- White to Off-White
- InChI
- InChI=1S/C19H19N3O3/c1-13(2)22-16(8-10-21-22)19-14(5-4-9-20-19)12-25-18-7-3-6-17(24)15(18)11-23/h3-11,13,24H,12H2,1-2H3
- InChIKey
- FWCVZAQENIZVMY-UHFFFAOYSA-N
- SMILES
- C(=O)C1=C(OCC2=CC=CN=C2C2N(C(C)C)N=CC=2)C=CC=C1O
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Voxelotor Usage And Synthesis
Uses
GBT 440 is a potent allosteric effector of sickle cell hemoglobin (Hb) that increases the affinity of Hb for oxygen and inhibits its polymerization when subjected to hypoxic conditions.
Biological Activity
Voxelotor improves the abnormal aggregation of hemoglobin under hypoxic conditions, which is the main cause of sickle cell disease-related red blood cell dysfunction, by forming a Schiff base with the N-terminal valine of the hemoglobin alpha chain, increasing the affinity of sickle cell hemoglobin for oxygen and preventing its aggregation.
Synthesis
below shows the synthesis route of Voxelotor
in vivo
| Animal Model: | HbSS Townes knock-in sickle mice (SS mice)[1] |
| Dosage: | 100 and 150 mg/kg |
| Administration: | Oral administration; twice a day; for 9-12 days |
| Result: | Reduced haemolysis. |
| Animal Model: | C57BL/6J mice, Sprague-Dawley rats, Beagle dogs and Cynomolgus monkeys[1] |
| Dosage: | 70, 1.6, 1 and 1 mg/kg for mice, rats, dogs and monkeys, respectively 30, 7.2, 2.5 and 4.25 mg/kg for mice, rats, dogs and monkeys, respectively |
| Administration: | Intravenous (IV: 70, 1 6, 1 and 1 mg/kg, respectively) Oral (PO: 30, 7 2, 2 5 and 4 3 mg/kg, respectively) |
| Result: | 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. 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. |
References
[1] Patent: WO2013/102142, 2013, A1. Location in patent: Paragraph 0179
[2] Patent: WO2013/102142, 2013, A1. Location in patent: Paragraph 0178
VoxelotorSupplier
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