Voxelotor (GBT 440)
(Synonyms: 沃塞洛托,GBT 440) 目录号 : GC32434
A modulator of sickle hemoglobin
Cas No.:1446321-46-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GBT-440 is a modulator of sickle hemoglobin (HbS) that binds covalently to the N-terminal valine of the α chain of HbS.1 In vitro, GBT-440 increases HbS affinity for oxygen (EC50s = 8.2 and 415 μM for purified HbS and whole blood from sickle cell anemia patients, respectively) and delays oxygen release from and polymerization of HbS in a concentration-dependent manner. GBT-440 (100-150 mg/kg) increases red blood cell half-life and reduces sickling ex vivo in whole blood isolated from a murine model of sickle cell anemia. It also reduces ex vivo sickling of sickle cell trait red blood cells under conditions of hypoxia, acidosis, and dehydration.2
1.Oksenberg, D., Dufu, K., Patel, M.P., et al.GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell diseaseBr. J. Haematol.175(1)141-153(2016) 2.Dufu, K., Lehrer-Graiwer, J., Ramos, E., et al.GBT440 inhibits sickling of sickle cell trait blood under in vitro conditions mimicking strenuous exerciseHematol. Rep.8(3)6637(2016)
| Cas No. | 1446321-46-5 | SDF | |
| 别名 | 沃塞洛托,GBT 440 | ||
| Canonical SMILES | OC1=CC=CC(OCC2=C(C3=CC=NN3C(C)C)N=CC=C2)=C1C=O | ||
| 分子式 | C19H19N3O3 | 分子量 | 337.37 |
| 溶解度 | DMSO : ≥ 125 mg/mL (370.51 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Postmodification of Voxelotor (GBT 440) via [Rh]-catalyzed cross dehydrogenative coupling with olefins
Bioorg Med Chem Lett 2022 Dec 1;77:129022.PMID:36241050DOI:10.1016/j.bmcl.2022.129022.
The directed Rh(III)-catalyzed cross dehydrogenative coupling of the pyrazole unit of the GBT-440 scaffold has been explored with simple as well as conjugated olefins to synthesize post-functionalized GBT-440 analogues. The screening of these synthesized compounds for improving the oxygen binding efficiency of the hemoglobin isolated from the sickled red blood cells revealed that some of these compounds are as good as GBT-440.