GBT-440 | B3031

GTB-440 is a modulator of sickle hemoglobin S (HbS). It binds to the N‐terminal valine of one of the haemoglobin α chains and increases HbS affinity for oxygen. GBT440 dose‐dependently increases HbS affinity for oxygen (EC₅₀ = 8·2 μM) for purified HbS and (EC₅₀ = 415 μM) for whole blood from sickle cell disease (SCD) patients. It delays in vitro HbS polymerization and prevents sickling of RBCs. In a murine model of SCD, GBT-440 (100 and 150 mg/kg for 9–12 d) increases the half‐life of RBCs, reduces reticulocyte counts and prevents ex vivo RBC sickling.

GTB-440 is a modulator of sickle hemoglobin S (HbS). It binds to the N‐terminal valine of one of the haemoglobin α chains and increases HbS affinity for oxygen. GBT440 dose‐dependently increases HbS affinity for oxygen (EC₅₀ = 8·2 μM) for purified HbS and (EC₅₀ = 415 μM) for whole blood from sickle cell disease (SCD) patients. It delays in vitro HbS polymerization and prevents sickling of RBCs. In a murine model of SCD, GBT-440 (100 and 150 mg/kg for 9–12 d) increases the half‐life of RBCs, reduces reticulocyte counts and prevents ex vivo RBC sickling.

B3031 | GBT-440 DataSheet

Alternate Name/Synonyms: Voxelotor; Hemoglobin Modulators-1; 2-hydroxy-6-[[2-(2-propan-2-ylpyrazol-3-yl)pyridin-3-yl]methoxy]benzaldehyde; 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde; 2-hydroxy-6-((2-(1-(propan-2-yl)-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde; Benzaldehyde, 2-hydroxy-6-((2-(1-(1-methylethyl)-1H-pyrazol-5-yl)-3-pyridinyl)methoxy)-

Appearance: White to off-white solid powder

Formulation:

CAS Number: 1446321-46-5

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₁₉H₁₉N₃O₃

Molecular Weight: 337.37

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: ~33 mg/ml in DMSO and DMF, ~20 mg/ml in ethanol

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A modulator of sickle hemoglobin S (HbS)

MDL Number: MFCD29053764

PubChem CID: 71602803

SMILES: CC(C)N1C(=CC=N1)C2=C(C=CC=N2)COC3=CC=CC(=C3C=O)O

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

InChi Key: FWCVZAQENIZVMY-UHFFFAOYSA-N