RS 127445 HCl
(Synonyms: RS-127445; MT 500; RS127445) 目录号 : GC10670
5-HT2B receptor antagonist,high affinity
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
RS-127445 is a selective, high affinity 5-HT2B receptor antagonist.
The 5-HT2B receptor is a G-protein coupled receptor. 5-HT2B receptors are widely expressed in peripheral tissues of various species. 5-HT2B receptor expresses throughout the gastrointestinal tract including smooth muscle of the stomach fundus, oesophagus, colon and small intestine. The receptor has also been found in the placenta, uterus, lung and prostate. 5-HT2B receptors are present in many vascular beds and have been localized to both vascular smooth muscle and vascular endothelial cells [1].
RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) showed nanomolar affinity for the 5-HT2B receptor with the pKi of 9.5 ± 0.1. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pKB = 9.5 ± 0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4 ± 0.1). RS-127445 blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5 ± 1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9 ± 0.3). In rats, RS-127445 was bioavailable via the oral or intraperitoneal routes.
Reference:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al. RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.
| Cas No. | N/A | SDF | |
| 别名 | RS-127445; MT 500; RS127445 | ||
| 化学名 | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine hydrochloride | ||
| Canonical SMILES | FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31.Cl | ||
| 分子式 | C17H17ClFN3 | 分子量 | 317.79 |
| 溶解度 | ≥ 31.8mg/mL in DMSO | 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 | 3.1467 mL | 15.7337 mL | 31.4673 mL |
| 5 mM | 0.6293 mL | 3.1467 mL | 6.2935 mL |
| 10 mM | 0.3147 mL | 1.5734 mL | 3.1467 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。