产品
编 号:F746321
分子式:C19H20N2O4
分子量:340.37
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
联系客服
产品详情
生物活性:
GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia.

体内研究:
GBT1118 (70 or 140 mg/kg; oral; once) 增加小鼠对严重缺氧的耐受性。Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 10 mg/kg IV Administration of GBT1118MatrixT1/2 (h) AUC0-∞ (μg?h/mL) Vss (L/kg) CLs (mL/min/kg) Blood/Plasma Ratio
Blood13.929290.070.0651.4
Plasma11.3602.953.21
Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 100 mg/kg PO Administration of GBT1118MatrixTmax (h) Cmax (μg/mL) AUC0-∞ (μg?h/mL) F (%) Blood/Plasma Ratio
Blood23181342845.834.1
Plasma81222433.5
Animal Model:C57Bl/6 mice, acute hypoxia model
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
Dosage:10 or 100 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Showed good pharmacokinetic parameters.

体外研究:
GBT1118 通过亚胺中间体与血红蛋白 α 链的 N 端缬氨酸共价和可逆地结合,变构地增加细胞内血红蛋白对 O2 的亲和力。GBT1118 (样本血红蛋白浓度的 25%) 可保护红细胞在严重缺氧期间免受损伤。
产品资料