Bioactivity | GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia[1]. |
Invitro | 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[1] 的亲和力[1]。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[2]。 |
In Vivo | GBT1118 (70 or 140 mg/kg; oral; once) 增加小鼠对严重缺氧的耐受性[1]。Blood and plasma pharmacokinetic parameters of GBT1118 in male mice following 10 mg/kg IV Administration of GBT1118[1] Matrix |
Name | GBT1118 |
CAS | 1628799-51-8 |
Formula | C19H20N2O4 |
Molar Mass | 340.37 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [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. |