1628799-51-8

Name	Benzaldehyde, 2-hydroxy-6-[[(2S)-1-(3-pyridinylcarbonyl)-2-piperidinyl]methoxy]-
CAS	1628799-51-8
Molecular Formula	C19H20N2O4
Molecular Weight	340.37
MOL File	1628799-51-8.mol

Synonyms

GBT1118 Benzaldehyde, 2-hydroxy-6-[[(2S)-1-(3-pyridinylcarbonyl)-2-piperidinyl]methoxy]-

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Chemical Properties

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

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	T_1/2 (h)	AUC_0-∞ (μg?h/mL)	V_ss (L/kg)	CL_s (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	T_max (h)	C_max (μg/mL)	AUC_0-∞ (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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Telephone 15002134094

Websitehttps://www.targetmol.cn/

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