Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMY 7378 dihydrochloride (BMY7378 HCl) 是选择性 α1D 肾上腺素受体拮抗剂,也是5-HT1A 受体部分激动剂。它同表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM) 是同克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 的100 以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 198 | 现货 | ||
10 mg | ¥ 279 | 现货 | ||
25 mg | ¥ 493 | 现货 | ||
50 mg | ¥ 891 | 现货 | ||
100 mg | ¥ 1,630 | 现货 | ||
200 mg | ¥ 3,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 198 | 现货 |
产品描述 | BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor. |
靶点活性 | 5-HT1A:8.3(pIC50), α1D-adrenoceptor:8.2(pKi), 5-HT1C:6.4(pIC50), D2 receptor:7.4(pIC50), α2C-adrenoceptor:6.54(pKi) |
体外活性 | 在大鼠体内,BMY7378(0.25-5 mg/kg,s.c.)剂量依赖性降低8-OH-DPAT(0.75 mg/kg,s.c.)诱导的前爪踩踏和头部摇晃.在麻醉大鼠的腹侧海马体中,大鼠体内微量渗析检测显示,BMY7378使5-HT释放出现剂量依赖性的显著减少.BMY7378 (pA2为8.67)与去甲肾上腺素作用可使大鼠主动脉收缩,效果比育亨宾 (pA2为6.62)高约100倍.BMY7378 (pA2:6.48)会拮抗人体隐静脉(α2C-肾上腺素受体)中去甲肾上腺素引起的收缩响应,效果比育亨宾(pA2为7.56)低10倍. |
体内活性 | BMY7378对α1D-肾上腺素受体亚型的作用有选择性{PKi: α1b-肾上腺素受体6.2(仓鼠),7.2(人);α1c-肾上腺素受体 6.1(牛),6.6(人);α1d-肾上腺素受体8.2(大鼠),9.4(人)}。BMY7378对α2c-肾上腺素受体的选择性(pKi:6.54)是其他α2-肾上腺素受体的10倍。在大鼠中缝背核中,BMY7378(1-30 nM)具有剂量依赖性的抑制作用。 |
激酶实验 | Phosphatase activities are determined on immunoprecipitates of the phosphatases. Briefly, 2×106 K562 cells are treated for 18 hr with Salubrinal (20 μM), PSI (10 nM), the combination of both drugs or okadaic acid (100 nM). After washing with PBS, cells are lysed for 15 min on ice either in PP1LB (for determination of PP1γ-activity; 20 mM Tris-HCl, pH 7.5, 1% Triton X-100, 10% glycerol, 132 mM NaCl, Roche complete protease inhibitor ) or in RIPA (for PP2A), supplemented with Roche complete protease inhibitor). Cell lysates containing 500 μg (PP1γ) or 300 μg (PP2A) protein are immunoprecipitated overnight at 4°C with 2-3 μg of the appropriate antibodies and then incubated with Protein A-Sepharose. Immunoprecipitates are washed three times in lysis buffer, followed by resuspension in phosphatase assay buffer (PP2A: 20 mM Tris-HCl, pH7.5, 0.1 mM CaCl2; PP1γ: 50 mM Tris HCl pH 7.0, 0.2 mM MnCl2, 0.1 mM CaCl2, 125 μg/mL BSA, 0.05% Tween 20), supplemented with 100 μM 6,8-difluoro-4-methyl-umbelliferyl phosphate (DiFMUP). Precipitates are allowed to react with substrate for 1 hr at 37°C on an Eppendorf Thermoshaker, centrifuged and DiFMU fluorescence is measured on a BioTek Lambda Fluoro 320 microplate reader (360 nmex/460 nmem). Phosphatase activities are given as percent change relative to the control (DMSO treated cells)[1]. |
别名 | BMY7378 HCl |
分子量 | 458.42 |
分子式 | C22H33Cl2N3O3 |
CAS No. | 21102-95-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 16 mg/mL (34.9 mM)
DMSO: 85 mg/mL (185.4 mM)
H2O: 84 mg/mL (183.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO / H2O | 1 mM | 2.1814 mL | 10.907 mL | 21.8141 mL | 54.5351 mL |
5 mM | 0.4363 mL | 2.1814 mL | 4.3628 mL | 10.907 mL | |
10 mM | 0.2181 mL | 1.0907 mL | 2.1814 mL | 5.4535 mL | |
20 mM | 0.1091 mL | 0.5454 mL | 1.0907 mL | 2.7268 mL | |
DMSO / H2O | 50 mM | 0.0436 mL | 0.2181 mL | 0.4363 mL | 1.0907 mL |
100 mM | 0.0218 mL | 0.1091 mL | 0.2181 mL | 0.5454 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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