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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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥413 有现货
10MG ¥599 有现货
25MG ¥988 有现货
50MG ¥1604 有现货
100MG ¥2989 有现货
200MG ¥4447 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    GBT-440
  • 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
  • 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。
  • 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.
  • 体外实验
    ——
  • 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.
  • 同义词
    GBT 440 | GBT440 | Voxelotor
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Other Targets
  • 研究领域
    Other Indications
  • 适应症
    Anemia

化学信息

  • CAS Number
    1446321-46-5
  • 分子量
    337.3725
  • 分子式
    C19H19N3O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    O=CC1=C(OCC2=CC=CN=C2C3=CC=NN3C(C)C)C=CC=C1O
  • 化学全称
    Benzaldehyde, 2-hydroxy-6-[[2-[1-(1-methylethyl)-1H-pyrazol-5-yl]-3-pyridinyl]methoxy]-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 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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