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Voxelotor (Synonyms: GBT 440)

Cat. No.: HY-18681 Purity: 99.96%
Handling Instructions

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.

Voxelotor Chemical Structure

Voxelotor Chemical Structure

CAS No. : 1446321-46-5

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Description

Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment[1].

IC50 & Target

HbS polymerization[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

337.37

Formula

C₁₉H₁₉N₃O₃

CAS No.

1446321-46-5

SMILES

OC1=CC=CC(OCC2=C(C3=CC=NN3C(C)C)N=CC=C2)=C1C=O

Shipping

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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (296.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9641 mL 14.8205 mL 29.6410 mL
5 mM 0.5928 mL 2.9641 mL 5.9282 mL
10 mM 0.2964 mL 1.4821 mL 2.9641 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  1% DMSO    99% saline

    Solubility: 0.5 mg/mL (1.48 mM); Suspended solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

  • 6.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.96%

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Keywords:

VoxelotorGBT 440GBT440GBT-440OthershaemoglobinHbSpolymerizationsicklecelldiseaseSCDInhibitorinhibitorinhibit

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Voxelotor
Cat. No.:
HY-18681
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