CWHM-1552
目录号 : GC35760
CWHM-1552 是一种口服有效的恶性疟原虫抑制剂，对 3D7 和 Dd2 strain 的 IC50s 分别是 51 nM and 53 nM。
Cas No.:2368253-58-9
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
CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively[1]. IC50: 51 nM (3D7 strain) and 53 nM (Dd2 strain)[1]
CWHM-1552 (Compound (-)-32a) (orally; 3-30 mg/kg/day for 4 days) inhibits parasitemia at 99.9% at 30 mg/kg/day and 94% at 10 mg/kg/day[1]. CWHM-1552 (i.v. administration; 2 mg/kg/day for 48 hours) has respectable half-lives (2.7 h) and low clearance in mice[1]. CWHM-1552 has good pharmacokinetic properties and oral efficacy in a mouse model of malaria. CWHM-1552 has an in vivo ED90 of P. chabaudi ASS infected Mice[1]
[1]. Meyers MJ, et al. 4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-N-(4-arylpyrrolidin-3-yl) acetamides. ACS Med Chem Lett. 2019 May, 10(6):966-971.
| Cas No. | 2368253-58-9 | SDF | |
| Canonical SMILES | CN(C)C1=CC=C(CC(N[C@@H]2CNC[C@H]2C3=CC=C(C(F)(C)F)C=C3)=O)C=C1 | ||
| 分子式 | C22H27F2N3O | 分子量 | 387.47 |
| 溶解度 | Soluble in DMSO | 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 | 2.5808 mL | 12.9042 mL | 25.8084 mL |
| 5 mM | 0.5162 mL | 2.5808 mL | 5.1617 mL |
| 10 mM | 0.2581 mL | 1.2904 mL | 2.5808 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。
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl- N-(4-arylpyrrolidin-3-yl)acetamides
ACS Med Chem Lett 2019 May 28;10(6):966-971.PMID:31223456DOI:PMC6580545
Malaria is caused by infection from the Plasmodium parasite and kills hundreds of thousands of people every year. Emergence of new drug resistant strains of Plasmodium demands identification of new drugs with novel chemotypes and mechanisms of action. As a follow up to our evaluation of 4-aryl-N-benzylpyrrolidine-3-carboxamides as novel pyrrolidine-based antimalarial agents, we describe herein the structure-activity relationships of the reversed amide homologues 2-aryl-N-(4-arylpyrrolidin-3-yl)acetamides. Unlike their carboxamide homologues, acetamide pyrrolidines do not require a third chiral center to be potent inhibitors of P. falciparum and have good pharmacokinetic properties and improved oral efficacy in a mouse model of malaria. Compound (-)-32a (CWHM-1552) has an in vitro IC50 of 51 nM in the P. falciparum 3D7 assay and an in vivo ED90 of <10 mg/kg/day and ED99 of 30 mg/kg/day in a murine P. chabaudi model. Remarkably, the absolute stereochemical preference for this acetamide series (3S,4R) is opposite of that determined for the homologous carboxamide series. Lead compounds for this class have modest affinities for the hERG channel and inhibit CYP 3A4. Additional optimization is needed in order to eliminate these undesired properties from this otherwise promising series of antimalarial compounds.