RS 67506 hydrochloride
目录号 : GC14696
potent and selective 5-HT4 partial agonist
Cas No.:168986-61-6
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
pKi: 8.8
RS 67506 hydrochloride is a potent and selective 5-HT4 partial agonist.
Selective agonists of 5-HT4 receptor can not only enhance congnitive performance, facilitate gastrointestinal motility, and also correct micturation disturbances which is associated with detrusor hypomotilityor actas analgesics.
In vitro: RS 67506 acted as a potent partial agonist with respect to 5-HT at the 5-HT4 receptor regulating relaxation of the carbachol-precontracted oesophagus. Relaxant responses to RS 67506 was surmountably antagonized with apparent affinities (pKB) of 9.0. RS 67506, therefore, acted as potent, partial 5-HT4 receptor agonists in vitro. The compound may have been used in elucidating the physiological role in 5-HT4 receptors by virtue of their high potency and selectivity [1].
In vivo: RS 67506 induced dose-dependent potentiates heart rate of the anaesthetized micropig (ED50 5.4 pg kg-1, i.v.) with maximal increases of 47 beats min-1 [1]. In addition, in a rat model of spatial learning and memory, the effects of two novel potent and selective 5-HT4 receptor agonists (RS67333 and RS67506) were studied. By contrast, there was no effect seen to RS67506 (0.1, 10 and 1000 pg/kg, i.p.) of equivalent potency and selectivity to RS67333.This differential result may suggest the enhanced ability of RS67333 to enter the CNS, with respect to RS67506 [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1]. Eglen RM, Bonhaus DW, Johnson LG, Leung E, Clark RD. Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo. Br J Pharmacol. 1995 Aug;115(8):1387-92.
[2]. Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM. The effects of novel, selective 5-hydroxytryptamine (5-HT) 4 receptor ligands in rat spatial navigation. Neuropharmacology. 1997 Apr-May;36(4-5):689-96.
| Cas No. | 168986-61-6 | SDF | |
| 化学名 | N-(2-(4-(3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl)piperidin-1-yl)ethyl)methanesulfonamide hydrochloride | ||
| Canonical SMILES | ClC(C=C(C(OC)=C1)C(CCC2CCN(CCNS(=O)(C)=O)CC2)=O)=C1N.Cl | ||
| 分子式 | C18H28ClN3O4S.HCl | 分子量 | 454.41 |
| 溶解度 | Soluble to 80 mM in Water | 储存条件 | Store 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2007 mL | 11.0033 mL | 22.0066 mL |
| 5 mM | 0.4401 mL | 2.2007 mL | 4.4013 mL |
| 10 mM | 0.2201 mL | 1.1003 mL | 2.2007 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。