Voxelotor
Based on 9 publication(s) in Google Scholar
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 1446321-46-5
- Formula: C19H19N3O3
- Molecular Weight:337.37
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Voxelotor
More- Am J Hematol. 2019 May;94(5):575-584. [Abstract]
- Pharmaceutics. 2021 Sep 2;13(9):1388. [Abstract]
- Sci Rep. 2020 Nov 20;10(1):20277. [Abstract]
- Anal Bioanal Chem. 2024 Nov;416(28):6575-6588. [Abstract]
- J Pharm Biomed Anal. 2023 Jan 20:223:115152. [Abstract]
- Drug Test Anal. 2025 Oct 9. [Abstract]
- Am J Clin Pathol. 2020 Oct 13;154(5):627-634. [Abstract]
- bioRxiv. 2025 May 15:2025.05.12.653546. [Abstract]
- Patent. US20220340531A1.
Biological Activity
HbS polymerization[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HbSS Townes knock-in sickle mice (SS mice)[1]
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Dosage:100 and 150 mg/kg
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Administration:Oral administration; twice a day; for 9-12 days
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Result:Reduced haemolysis.
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Animal Model:C57BL/6J mice, Sprague-Dawley rats, Beagle dogs and Cynomolgus monkeys[1]
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1446321-46-5
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Appearance Solid
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Molecular Weight 337.37
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Formula C19H19N3O3
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Color Off-white to light brown
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SMILES
OC1=CC=CC(OCC2=C(C3=CC=NN3C(C)C)N=CC=C2)=C1C=O
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Synonyms
GBT 440
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications (9)
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Journal Impact Factor
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Most Recent
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Am J Hematol
Rapid and reproducible characterization of sickling during automated deoxygenation in sickle cell disease patients. [Abstract]2019 May;94(5):575-584. PMID: 30784099 -
Pharmaceutics
Quality-by-Design-Based Development of a Voxelotor Self-Nanoemulsifying Drug-Delivery System with Improved Biopharmaceutical Attributes. [Abstract]2021 Sep 2;13(9):1388. PMID: 34575467 -
Sci Rep
VZHE-039, a novel antisickling agent that prevents erythrocyte sickling under both hypoxic and anoxic conditions. [Abstract]2020 Nov 20;10(1):20277. PMID: 33219275 -
Anal Bioanal Chem
Metabolic profile characterization of voxelotor in human urine based on in vivo and in vitro models for doping control. [Abstract]2024 Nov;416(28):6575-6588. PMID: 39365442 -
J Pharm Biomed Anal
Quantitative assessment of the in-vitro binding kinetics of antisickling aromatic aldehydes with hemoglobin A: A universal HPLC-UV/Vis method to quantitate Schiff-base adduct formation. [Abstract]2023 Jan 20:223:115152. PMID: 36399908 -
Drug Test Anal
Equine Metabolism of Voxelotor and Its Impact on Hematological Indices: A Doping Control Perspective. [Abstract]2025 Oct 9. PMID: 41063632 -
Am J Clin Pathol
Voxelotor Treatment Interferes With Quantitative and Qualitative Hemoglobin Variant Analysis in Multiple Sickle Cell Disease Genotypes. [Abstract]2020 Oct 13;154(5):627-634. PMID: 32561909 -
bioRxiv
2025 May 15:2025.05.12.653546. PMID: 40463219 -
Solvent & Solubility
DMSO : 100 mg/mL (296.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |
Voxelotor Related Classifications
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