Cevimeline hydrochloride hemihydrate
(Synonyms: 盐酸西维美林半水合物; SNI-2011; AF102B hydrochloride hemihydrate) 目录号 : GC17157
Cevimeline hydrochloride hemihydrate (SNI-2011) 是乙酰胆碱的奎宁环衍生物，是一种选择性和口服活性的毒蕈碱 M1 和 M3 受体激动剂。
Cas No.:153504-70-2
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
Cevimeline hydrochloride hemihydrate is a novel and selective agonist of muscarinic acetylcholine receptor [1].
Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors and mediate serous-saliva secretion and tear secretion. It is more sensitive to muscarine than nicotine [1].
Cevimeline hydrochloride hemihydrate induced contractions of isolated guinea pig ilea and trachea with EC50 values of 3.5 and 3 μM, respectively. Binding studies indicated that Cevimeline hydrochloride hemihydrate was a potent and highly selective M1-type muscarinic agonist. Also, it had a higher affinity for M1 receptors than other M1 agonists [2].
In normal rats and mice, X-irradiated saliva secretion defective rats and two strains of autoimmune disease mice, intraduodenal administrations of SNI-2011 (3-30 mg/kg) increased saliva and tear secretions in a dose-dependent way, which suggested that Cevimeline hydrochloride hemihydrate directly stimulated muscarinic receptors in salivary and lacrimal glands for saliva and tear secretions [1].
References:
[1]. Iga Y, Arisawa H, Ogane N, et al. (+/-)-cis-2-methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride, hemihydrate (SNI-2011, cevimeline hydrochloride) induces saliva and tear secretions in rats and mice: the role of muscarinic acetylcholine receptors. Jpn J Pharmacol, 1998, 78(3): 373-380.
[2]. Fisher A, Brandeis R, Karton I, et al. (+-)-cis-2-methyl-spiro(1,3-oxathiolane-5,3') quinuclidine, an M1 selective cholinergic agonist, attenuates cognitive dysfunctions in an animal model of Alzheimer's disease. J Pharmacol Exp Ther, 1991, 257(1): 392-403.
| Cas No. | 153504-70-2 | SDF | |
| 别名 | 盐酸西维美林半水合物; SNI-2011; AF102B hydrochloride hemihydrate | ||
| 化学名 | (2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride | ||
| Canonical SMILES | CC1OC2(CN3CCC2CC3)CS1.O.Cl | ||
| 分子式 | C10H20ClNO2S | 分子量 | 253.79 |
| 溶解度 | DMSO : 40mg/mL; Water : 40mg/mL | 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 | 3.9403 mL | 19.7013 mL | 39.4027 mL |
| 5 mM | 0.7881 mL | 3.9403 mL | 7.8805 mL |
| 10 mM | 0.394 mL | 1.9701 mL | 3.9403 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。