GSK962040
(Synonyms: GSK962040) 目录号 : GC16491
GSK962040 (GSK962040) 是一种小分子选择性胃动素受体激动剂，pEC50 为 7.9。
Cas No.:923565-21-3
Sample solution is provided at 25 µL, 10mM.
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GSK962040 is a first small-molecule agonist of motilin receptor with pEC50 value of 7.9 [1].
GSK962040 is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. In the in vitro assay using recombinant human motilin receptor, GSK962040 shows an excellent inhibition activity against motilin receptor with pEC50 value of 7.9. GSK962040 is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. In rabbit isolated gastric antrum, GSK962040 is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration. GSK962040 also induces the contraction of human-isolated stomach preparations at 10μM [1, 2].
References:
[1] Westaway S M, Brown S L, Fell S C M, et al. Discovery of N-(3-Fluorophenyl)-1-[(4-([(3 S)-3-methyl-1-piperazinyl] methyl) phenyl) acetyl]-4-piperidinamine (GSK962040), the First Small Molecule Motilin Receptor Agonist Clinical Candidate. Journal of medicinal chemistry, 2009, 52(4): 1180-1189.
[2] Sanger G J, Westaway S M, Barnes A A, et al. GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterology & Motility, 2009, 21(6): 657-e31.
| Cas No. | 923565-21-3 | SDF | |
| 别名 | GSK962040 | ||
| 化学名 | 1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone | ||
| Canonical SMILES | CC1CN(CCN1)CC2=CC=C(C=C2)CC(=O)N3CCC(CC3)NC4=CC(=CC=C4)F | ||
| 分子式 | C25H33FN4O | 分子量 | 424.55 |
| 溶解度 | DMSO : 100 mg/mL (235.54 mM; Need ultrasonic) | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3554 mL | 11.7772 mL | 23.5544 mL |
| 5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL |
| 10 mM | 0.2355 mL | 1.1777 mL | 2.3554 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet