
GBT-440
CAS No. 1446321-46-5
GBT-440 ( GBT 440 | GBT440 | Voxelotor )
产品货号. M11895 CAS No. 1446321-46-5
镰状细胞血红蛋白的一种新的有效变构效应物;增加血红蛋白对氧的亲和力,从而在缺氧条件下抑制其聚合。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥413 | 有现货 |
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10MG | ¥599 | 有现货 |
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25MG | ¥988 | 有现货 |
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50MG | ¥1604 | 有现货 |
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100MG | ¥2989 | 有现货 |
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200MG | ¥4447 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称GBT-440
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述镰状细胞血红蛋白的一种新的有效变构效应物;增加血红蛋白对氧的亲和力,从而在缺氧条件下抑制其聚合。
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产品描述A new potent allosteric effector of sickle cell hemoglobin; increases the affinity of hemoglobin for oxygen and consequently inhibits its polymerization when subjected to hypoxic conditions; orally bioavailable and partitions highly and favorably into the red blood cell with a RBC/plasma ratio of ~150.Anemia Phase 3 Clinical(In Vitro):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).(In Vivo):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.
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体外实验——
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体内实验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, 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.
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同义词GBT 440 | GBT440 | Voxelotor
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通路Others
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靶点Other Targets
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受体Other Targets
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研究领域Other Indications
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适应症Anemia
化学信息
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CAS Number1446321-46-5
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分子量337.3725
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分子式C19H19N3O3
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESO=CC1=C(OCC2=CC=CN=C2C3=CC=NN3C(C)C)C=CC=C1O
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化学全称Benzaldehyde, 2-hydroxy-6-[[2-[1-(1-methylethyl)-1H-pyrazol-5-yl]-3-pyridinyl]methoxy]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Metcalf B, et al. ACS Med Chem Lett. 2017 Jan 23;8(3):321-326.
2. Oksenberg D, et al. Br J Haematol. 2016 Oct;175(1):141-53.
3. Dufu K, et al. Hematol Rep. 2016 Sep 28;8(3):6637.
产品手册




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