ADX 10059 hydrochloride
目录号 : GC12460
Negative allosteric modulator at mGlu5
Cas No.:757949-98-7
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
ADX 10059 hydrochloride is a potent and selective negative allosteric modulator of mGlu5 receptor with IC50 value of 17.1 nM [1].
Metabotropic glutamate receptor 5 (mGlu5 receptor) is a G protein-coupled receptor and is a receptor for glutamate, which is a primary neurotransmitter involved in signaling in the central nervous system [2].
ADX 10059 hydrochloride is a potent and selective mGlu5 receptor negative allosteric modulator. In patients with migraine, ADX10059 caused pain-free response in 16.1% patients compared with placebo of 4.5% [1]. In patients with gastro-oesophageal reflux disease (GORD) underwent 24-h oesophageal pH-metry, ADX10059 (250 mg) significantly reduced the percentage of acid exposure time with pH < 4 from 7.2% to 3.6%. Also, ADX 10059 significantly decreased the duration and number of symptomatic reflux episodes and reduced oesophageal acid exposure [2].
References:
[1]. Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine Expert Opin Investig Drugs, 2010, 19(4): 555-561.
[2]. Keywood C, Wakefield M, Tack J. A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease. Gut, 2009, 58(9): 1192-1199.
| Cas No. | 757949-98-7 | SDF | |
| 化学名 | 2-((3-fluorophenyl)ethynyl)-4,6-dimethylpyridin-3-amine hydrochloride | ||
| Canonical SMILES | CC1=CC(C)=NC(C#CC2=CC(F)=CC=C2)=C1N.Cl | ||
| 分子式 | C15H13FN2.HCl | 分子量 | 276.74 |
| 溶解度 | <6.92mg/ml in Water; <27.67mg/ml in DMSO | 储存条件 | Desiccate at RT |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6135 mL | 18.0675 mL | 36.135 mL |
| 5 mM | 0.7227 mL | 3.6135 mL | 7.227 mL |
| 10 mM | 0.3614 mL | 1.8068 mL | 3.6135 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。