SR 146131
目录号 : GC31613
SR146131是一种有效，有口服活性，选择性的非多肽缩胆囊素1(cholecystokinin1)受体激动剂。
Cas No.:221671-61-0
Sample solution is provided at 25 µL, 10mM.
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SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
SR 146131 inhibits in the binding of [125I]-BH-CCK-8S to CCK1sites on 3T3-hCCK1 cell membranes with an IC50 value of 0.56 ± 0.10 nM. At much higher concentrations, SR 146131 also inhibits the binding of radiolabeled CCK to CCK2sites in CHO-hCCK2 membranes with an IC50 of 162 ± 27 nM. SR 146131 is a potent CCK1 agonist on several intracellular events linked to CCK1 receptor activation in various cell types: on [Ca2+]i release and IP1 formation, SR 146131 appears as a full CCK1 receptor agonist in the 3T3-hCCK1 cells, but a partial CCK1receptor agonist on MAPK activation and early gene expression in this cell line. SR 146131 also acts as a partial agonist in the two neuroblastoma cell lines[1].
SR 146131 completely inhibits gastric and gallbladder emptying in mice (ED50 of 66 and 2.7 μg/kg p.o., respectively). SR 146131 dose dependently reduces food intake in fasted rats (from 0.1 mg/kg p.o.), in nonfasted rats in which food intake has been highly stimulated by the administration of neuropeptide Y (1-36) (from 0.3 mg/kg p.o.), in fasted gerbils (from 0.1 mg/kg p.o.), and in marmosets maintained on a restricted diet (from 3 mg/kg p.o.). SR 146131 (10 mg/kg p.o.) also increases the number of Fos-positive cells in the hypothalamic paraventricular nucleus of rats. Locomotor activity of mice is reduced by orally administered SR 146131 (from 0.3 mg/kg p.o.)[1].
[1]. Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51. [2]. Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization. J Pharmacol Exp Ther. 1999 May;289(2):752-61.
Cell experiment: | 3T3-hCCK1 cells grown to subconfluence in 6-well cluster plates are washed with fresh medium. Twenty-four hours later, the cells are stimulated for 15 min with various concentrations of CCK-8S or SR 146131[1]. |
Animal experiment: | Rats[1]Male Sprague-Dawley rats are fasted for 18 h, and allowed access to food for only 6 h between 10 AM and 4 PM each day. Water is available ad libitum. At the end of this adaptation phase, rats are administered SR 146131 (0.03-3 mg/kg p.o.). One hour after SR 146131 administration, a weighed amount of food is introduced into the cage, and food intake is measured 1, 3, 6, and 23 h after SR 146131 administration[1].Mice[1] SR 146131 (0.01-1 pg) is solubilized in DMSO (1 mg/mL), diluted to the required concentrations with water, and injected (in 1 μL) into one striatum in awake, hand-restrained female CD1 mice (25-30 g). After injection, the animals are placed individually in Plexiglas cages (10 × 10 × 15 cm). Turning behavior in mice is monitored[1]. |
References: [1]. Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51. | |
| Cas No. | 221671-61-0 | SDF | |
| Canonical SMILES | O=C(O)CN1C(C(NC2=NC(C3=CC(OC)=C(Cl)C=C3OC)=C(CCC4CCCCC4)S2)=O)=CC5=C1C(C)=CC(C)=C5 | ||
| 分子式 | C32H36ClN3O5S | 分子量 | 610.16 |
| 溶解度 | DMSO : 250 mg/mL (409.73 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6389 mL | 8.1946 mL | 16.3891 mL |
| 5 mM | 0.3278 mL | 1.6389 mL | 3.2778 mL |
| 10 mM | 0.1639 mL | 0.8195 mL | 1.6389 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