MMG-0358
目录号 : GC47694
An inhibitor of IDO1
Cas No.:1378976-02-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MMG-0358 is an inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50s = 2 and 80 nM for the mouse and human enzyme, respectively).1,2 It is selective for IDO1 over tryptophan 2,3-dioxygenase (TDO; IC50s = >100 µM for mouse and human TDO).1
1.RÖhrig, U.F., Majjigapu, S.R., Grosdidier, A., et al.Rational design of 4-aryl-1,2,3-triazoles for indoleamine 2,3-dioxygenase 1 inhibitionJ. Med. Chem.55(11)5270-5290(2012) 2.RÖhrig, U.F., Reynaud, A., Majjigapu, S.R., et al.Inhibition mechanisms of indoleamine 2,3-dioxygenase 1 (IDO1)J. Med. Chem.62(19)8784-8795(2019)
| Cas No. | 1378976-02-3 | SDF | |
| Canonical SMILES | ClC1=CC=C(O)C(C2=CN=NN2)=C1 | ||
| 分子式 | C8H6ClN3O | 分子量 | 195.6 |
| 溶解度 | DMF: 20mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2mg/mL,DMSO: 15mg/mL,Ethanol: 15mg/mL | 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 | 5.1125 mL | 25.5624 mL | 51.1247 mL |
| 5 mM | 1.0225 mL | 5.1125 mL | 10.2249 mL |
| 10 mM | 0.5112 mL | 2.5562 mL | 5.1125 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。
Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1)
J Med Chem 2019 Oct 10;62(19):8784-8795.PMID:31525930DOI:10.1021/acs.jmedchem.9b00942
Indoleamine 2,3-dioxygenase 1 (IDO1) catalyzes the rate-limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging. Its implication in pathologies such as cancer and neurodegenerative diseases has stimulated the development of IDO1 inhibitors. However, negative phase III clinical trial results of the IDO1 inhibitor epacadostat in cancer immunotherapy call for a better understanding of the role and the mechanisms of IDO1 inhibition. In this work, we investigate the molecular inhibition mechanisms of four known IDO1 inhibitors and of two quinones in detail, using different experimental and computational approaches. We also determine for the first time the X-ray structure of the highly efficient 1,2,3-triazole inhibitor MMG-0358. Based on our results and a comprehensive literature overview, we propose a classification scheme for IDO1 inhibitors according to their inhibition mechanism, which will be useful for further developments in the field.