MTEP hydrochloride
(Synonyms: 3-[2-(2-甲基-4-噻唑基)乙炔基]吡啶盐酸盐) 目录号 : GC11871
A selective mGlu5a receptor antagonist
Cas No.:1186195-60-7
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
IC50: 5 nM
MTEP is a selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonist.
The mGluRs are classified into three groups: group I (mGluR1 and 5), group II (mGluR2 and 3) and group III (mGluR4, 6, 7 and 8). mGluR5 belonging to group I is excitatory, mainly localized at the edge of axo-spinous and axodendritic synaptic junctions.
In vitro: Like MPEP, MTEP showed a nanomolar affinity for mGluR5, but seemed to be superior to MPEP in term of specificity. MTEP did not influence mGluR2, mGluR7, NMDA, AMPA or kainate receptors, while inhibited MAOA at a concentration three times higher than MPEP. Moreover, recent study indicated that MTEP was five times stronger that MPEP as an anxiolytic compound [1].
In vivo: MTEP with doses between 0.5 and 3 mg/kg was found to decrease the haloperidol-induced muscle rigidity, which was measured as an increased muscle resistance of the rat hind leg. The longest and strongest effect was observed with the dose of 1 mg/kg. MTEP was also found to reduce the haloperidol-induced increase in electromyographic activity recorded in the tibialis anterior and gastrocnemius muscles. 3 and 5 mg/kg of MTEP could inhibit the haloperidol- induced catalepsy [1].
Clinical trial: N/A
Reference:
[1] Ossowska K,Konieczny J,Wolfarth S,Pilc A. MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats. Neuropharmacology.2005 Sep;49(4):447-55.
| Cas No. | 1186195-60-7 | SDF | |
| 别名 | 3-[2-(2-甲基-4-噻唑基)乙炔基]吡啶盐酸盐 | ||
| 化学名 | 2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole;hydrochloride | ||
| Canonical SMILES | CC1=NC(=CS1)C#CC2=CN=CC=C2.Cl | ||
| 分子式 | C11H9ClN2S | 分子量 | 236.72 |
| 溶解度 | DMF: 3 mg/ml,DMSO: 15 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 10 mg/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 | 4.2244 mL | 21.122 mL | 42.244 mL |
| 5 mM | 0.8449 mL | 4.2244 mL | 8.4488 mL |
| 10 mM | 0.4224 mL | 2.1122 mL | 4.2244 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。