Voxelotor

目录号: PL04824 纯度: ≥99%
Voxelotor (GBT 440) 是一种有效的镰状血红蛋白 (HbS) 聚合抑制剂。Voxelotor 有潜力用于镰状细胞贫血病的研究。
CAS No. :1446321-46-5
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中文名称
Voxelotor
中文别名
GBT 440
英文名称
Voxelotor
英文别名
GBT 440;Voxelotor;GBT-440;Voxelotor(GBT440, GTX011);Hemoglobin Modulators-1;3ZO554A4Q8;Voxelotor [USAN];Voxelotor (USAN);2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde;GBT440;FWCVZAQENIZVMY-UHFFFAOYSA-N;BCP20182;BDBM50235297;SB19656;2-hydroxy-6-[[2-(2-propan-2-ylpyrazol-3-yl)pyridin-3-yl]methoxy]benzaldehyde;AK547400;S8540;D11330
Cas No.
1446321-46-5
分子式
C19H19N3O3
分子量
337.37
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
详情描述
Voxelotor (GBT 440) 是一种有效的镰状血红蛋白 (HbS) 聚合抑制剂。Voxelotor 有潜力用于镰状细胞贫血病的研究。
产品详情
Voxelotor (GBT 440) 是一种有效的镰状血红蛋白 (HbS) 聚合抑制剂。Voxelotor 有潜力用于镰状细胞贫血病的研究。
生物活性
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
性状
Solid
IC50 & Target[1][2]
HbS polymerization
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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 T 1/2 s 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 C max s 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (296.41 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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