货号	规格	价格	上海	北京	珠海	武汉
S83367-5mg	99.80%	￥360.00 S83367-5mg ￥360.00 现货	9 9	-	-	-
S83367-10mg	99.80%	￥595.00 S83367-10mg ￥595.00 现货	9 9	-	-	-
S83367-50mg促销	99.80%	￥1780.00 ￥1420.00 S83367-50mg ￥1420.00 现货	7 7	-	-	-

货号

规格

价格

上海

北京

珠海

武汉

购买数量

S83367-5mg

99.80%

￥360.00

S83367-10mg

99.80%

￥595.00

S83367-50mg促销

99.80%

￥1780.00 ￥1420.00

产品描述：

Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment

靶点：

HbS polymerization;Others

体外研究：

Voxelotor (GBT440) binds to the N-terminal a chain of haemoglobin (Hb), increases haemoglobin S (HbS) affinity for oxygen, delays in vitro HbS polymerization and prevents sickling of red blood cells (RBCs)

体内研究：

Voxelotor (GBT440; 100-150 mg/kg; administered twice a day by oral gavage for 9-12 days) reduces ex vivo sickling and prolongs red blood cells (RBCs) half-life in a murine model of sickle cell disease (SCD). Voxelotor shows T1/2s of 11.7, 19.1±1.5, 66.0±11, 28.8±4.0 hours for mouse (70 mg/kg; i.v.), rat (1.6 mg/kg; i.v.), dog (1 mg/kg; i.v.), and momkey (1 mg/kg; i.v.), respectively. Voxelotor shows Cmaxs of 81.9, 71.2±6.0, 5.56±1.6, and 25.2±5.5 μg/mL for mouse (30 mg/kg; p.o.), rat (7.2 mg/kg; p.o.), dog (2.5 mg/kg; p.o.), and momkey (4.25 mg/kg; p.o.), respectively. Animal Model: HbSS Townes knock-in sickle mice (SS mice) Dosage: 100 and 150 mg/kg Administration: Oral administration; twice a day; for 9-12 days Result: Reduced haemolysis. Animal Model: C57BL/6J mice, Sprague-Dawley rats, Beagle dogs and Cynomolgus monkeys Dosage: 70, 1.6, 1 and 1 mg/kg for mice, rats, dogs and monkeys, respectively30, 7.2, 2.5 and 4.25 mg/kg for mice, rats, dogs and monkeys, respectively Administration: Intravenous (IV: 70, 1 6, 1 and 1 mg/kg, respectively)Oral (PO: 30, 7 2, 2 5 and 4 3 mg/kg, respectively) Result: T1/2s of 11.7, 19.1±1.5, 66.0±11, 28.8±4.0 hours for mouse (70 mg/kg; i.v.), rat (1.6 mg/kg; i.v.), dog (1 mg/kg; i.v.), and momkey (1 mg/kg; i.v.), respectively.Cmaxs of 81.9, 71.2±6.0, 5.56±1.6, and 25.2±5.5 μg/mL for mouse (30 mg/kg; p.o.), rat (7.2 mg/kg; p.o.), dog (2.5 mg/kg; p.o.), and momkey (4.25 mg/kg; p.o.), respectively.

参考文献：

1. Oksenberg D, et al. GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell disease. Br J Haematol. 2016 Oct;175(1):141-53. 2. Metcalf B, Chuang C, Dufu K, et al. Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. ACS Med Chem Lett. 2017;8(3):321-326.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.964 ml	14.82 ml	29.641 ml
5 mM	0.593 ml	2.964 ml	5.928 ml
10 mM	0.296 ml	1.482 ml	2.964 ml
50 mM	0.059 ml	0.296 ml	0.593 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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