| Identification | Back Directory | [Name]
Benzaldehyde, 2-hydroxy-6-[[(2S)-1-(3-pyridinylcarbonyl)-2-piperidinyl]methoxy]- | [CAS]
1628799-51-8 | [Synonyms]
GBT1118
Benzaldehyde, 2-hydroxy-6-[[(2S)-1-(3-pyridinylcarbonyl)-2-piperidinyl]methoxy]- | [Molecular Formula]
C19H20N2O4 | [MOL File]
1628799-51-8.mol | [Molecular Weight]
340.37 |
| Chemical Properties | Back Directory | [Boiling point ]
552.4±35.0 °C(Predicted) | [density ]
1.273±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
7.81±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia[1]. | [in vivo]
GBT1118 (70 or 140 mg/kg; oral; once) increases tolerance to severe hypoxia in mice[1].
Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 10 mg/kg IV Administration of GBT1118[1]
| Matrix | T1/2 (h) | AUC0-∞ (μg?h/mL) | Vss (L/kg) | CLs (mL/min/kg) | Blood/Plasma Ratio | | Blood | 13.9 | 2929 | 0.07 | 0.06 | 51.4 | | Plasma | 11.3 | 60 | 2.95 | 3.21 | |
Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 100 mg/kg PO Administration of GBT1118[1]| Matrix | Tmax (h) | Cmax (μg/mL) | AUC0-∞ (μg?h/mL) | F (%) | Blood/Plasma Ratio | | Blood | 2 | 318 | 13428 | 45.8 | 34.1 | | Plasma | 8 | 12 | 224 | 33.5 | |
| Animal Model: | C57Bl/6 mice, acute hypoxia model[1] | | Dosage: | 70 or 140 mg/kg | | Administration: | Oral, single dose | | Result: | Improved tolerance to 5% O2 hypoxia exposure. Increased O2 delivery during hypoxia, thus preserving MAP, HR, blood flow, and aerobic metabolism. Increased blood O2 loading in the lungs and allowed for increased O2 delivery during hypoxia. Decreased hypoxia in vital tissues and lowered lactate levels. |
| Animal Model: | C57Bl/6 mice[1] | | Dosage: | 10 or 100 mg/kg | | Administration: | IV or PO (Pharmacokinetic Analysis) | | Result: | Showed good pharmacokinetic parameters. |
| [References]
[1] Dufu K, et al. GBT1118, a potent allosteric modifier of hemoglobin O2 affinity, increases tolerance to severe hypoxia in mice. Am J Physiol Heart Circ Physiol. 2017 Aug 1;313(2):H381-H391. DOI:10.1152/ajpheart.00772.2016
[2] Tarasev M, et al. GBT1118, a voxelotor analog, protects red blood cells from damage during severe hypoxia. Am J Transl Res. 2022 Jan 15;14(1):240-251. PMID:35173841 |
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