Methapyrilene (hydrochloride)
(Synonyms: 盐酸美沙吡林,Thenylpyramine hydrochloride) 目录号 : GC48805
An H1 receptor antagonist and non-genotoxic carcinogen
Cas No.:135-23-9
Sample solution is provided at 25 µL, 10mM.
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Methapyrilene is a histamine H1 receptor antagonist (Ki = 4.5 nM) and non-genotoxic carcinogen.1,2 Dietary administration of methapyrilene (0.1%) induces liver tumors in rats, with greater than 50% of rats incurring distant metastases.3 It decreases the acetylation of histone 3 lysine 9 (H3K9) and H3K56, as well as the di- and trimethylation of H3K4 and H4K20, respectively, in rat liver when administered at 40 mg/kg per day for six weeks.2 Methapyrilene also increases 4-hydroxy nonenal (4-NHE) protein adducts in rat liver. Formulations containing methapyrilene were previously used as sleep aids.
1.Tran, V.T., Chang, R.S.L., and Snyder, S.H.Histamine H1 receptors identified in mammalian brain membranes with [3H]mepyramineProc. Natl. Acad. Sci. U.S.A.75(12)6290-6294(1978) 2.Shpyleva, S., Dreval, K., de Conti, A., et al.Editor's highlight: Organ-specific epigenetic changes induced by the nongenotoxic liver carcinogen methapyrilene in fischer 344 ratsToxicol. Sci.156(1)190-198(2017) 3.Lijinsky, W., Reuber, M.D., and Blackwell, B.N.Liver tumors induced in rats by oral administration of the antihistaminic methapyrilene hydrochlorideScience209(4458)817-819(1980)
| Cas No. | 135-23-9 | SDF | |
| 别名 | 盐酸美沙吡林,Thenylpyramine hydrochloride | ||
| Canonical SMILES | CN(C)CCN(CC1=CC=CS1)C2=NC=CC=C2.Cl | ||
| 分子式 | C14H19N3S•HCl | 分子量 | 297.8 |
| 溶解度 | DMF: 15 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | -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 | 3.358 mL | 16.7898 mL | 33.5796 mL |
| 5 mM | 0.6716 mL | 3.358 mL | 6.7159 mL |
| 10 mM | 0.3358 mL | 1.679 mL | 3.358 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