HTL14242
HTL14242 is a mGlu5 Negative Allosteric Modulator. Metabotropic glutamate receptors (mGluRs) constitute the class C of G-protein coupled receptors (GPCRs) and play a key role in glutamatergic signaling. The inhibition of mGluR5, which is mostly expressed in the striatum, hippocampus, amygdala, and frontal cortex, is therefore considered as a potential therapeutic intervention in a number of psychiatry indications, including fragile X syndrome, anxiety, and depression.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | HTL14242 |
|---|---|
| Iupac 化学名称 | 3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile |
| 同义词 | HTL14242; HTL-14242; HTL 14242; HTL0014242; TMP-301 |
| 英文同义词 | HTL14242; HTL-14242; HTL 14242; HTL0014242; TMP-301 |
| 分子式 | C16H8ClFN4 |
| 分子量 | 310.71 |
| Smile | N#CC1=CC(C2=NC=NC(C3=NC=C(F)C=C3)=C2)=CC(Cl)=C1 |
| InChiKey | FQAXDSVNYVVQSE-UHFFFAOYSA-N |
| InChi | InChI=1S/C16H8ClFN4/c17-12-4-10(7-19)3-11(5-12)15-6-16(22-9-21-15)14-2-1-13(18)8-20-14/h1-6,8-9H |
| Cas号 | 1644645-32-8 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 0-4℃，可保存几天到几周；-20℃，可保存 几个月。 |
| 可溶性 | 溶于DMSO等有机溶剂 |
| 处理方式 | |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall
FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. Fragment and
Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5
Negative Allosteric Modulator HTL14242
(3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile). J Med Chem.
2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. PubMed PMID:
26225459.
2: Topiol S, Sabio M. 7TM X-ray structures for class C GPCRs as new
drug-discovery tools. 1. mGluR5. Bioorg Med Chem Lett. 2016 Jan 15;26(2):484-94.
doi: 10.1016/j.bmcl.2015.11.087. PubMed PMID: 26706173.
3: Tehan BG, Christopher JA. The use of conformationally thermostabilised GPCRs
in drug discovery: application to fragment, structure and biophysical techniques.
Curr Opin Pharmacol. 2016 Oct;30:8-13. doi: 10.1016/j.coph.2016.06.010. Review.
PubMed PMID: 27400445.
