Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LY2119620 是人 M2 和 M4 毒蕈碱乙酰胆碱受体的特异性变构激动剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 429 | 现货 | ||
2 mg | ¥ 619 | 现货 | ||
5 mg | ¥ 957 | 现货 | ||
10 mg | ¥ 1,620 | 现货 | ||
25 mg | ¥ 3,230 | 现货 | ||
50 mg | ¥ 4,770 | 现货 | ||
100 mg | ¥ 6,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 997 | 现货 |
产品描述 | LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
体外活性 | LY2119620 displays modest allosteric agonism and positively modulates the functional G protein–signaling ability of an agonist at the M2/M4 receptor subtypes by placing the M2 and M4 receptors into an active G protein–bound state. LY2119620 enhances the potency of three muscarinic acetylcholine receptor agonists, ACh, Oxo-M and iperoxo. [1] [3H]LY2119620 can be used as a probe for the human M(2) and M(4) muscarinic receptor allosteric binding sites. [2] |
激酶实验 | Biochemical Assay: For IC50 determination, EI1 is serial diluted threefold in DMSO for a total of 12 concentrations, with the starting concentration at 1 μM. The reaction is incubated at room temperature for 120 min, and stopped by adding quench solution (2.5% TFA with 320 nM d4-SAH). SAH production is quantitated using an API 4000 triple quadrupole mass spectrometry with Turbulon Spray coupled with Prominence UFLC. The percentage of inhibition is normalized using positive (no inhibitor) and negative (no enzyme) controls, and IC50 calculated using PRISM. Enzymology studies of S-Adenosyl methionine (SAM) competition are performed with slight modification of reaction condition: 10 μM EI1 is used as the starting dose for serial dilution. SAM is titrated over a range between 1 μM and 50 μM (corresponding to 1 × Km and 50 × Km), and substrate peptide is present in the final reaction mixture at its saturated condition (10 μM). For histone methyltransferase (HMT) profiling in Table 1, all HMTs are purified recombinant proteins from either Escherichia coli or Baculovirus system. The catalytic domain of G9a, SuV39H2, Set7/9, CARM1, SETD8, NSD3, SETD2, and Dot1L, and the full-length SmyD2 protein were used in the biochemical assays. HMT biochemical reactions are carefully characterized with enzymology studies and the SAM and substrate Km determined. The SAM and substrate concentrations are kept at their respective Km for most of the HMTs, except the ones (SmyD2 and Set7/9) with low SAM-Km value, for which 0.5 μM SAM is used. All HMT reactions are performed using the same assay format where the production of SAH from the biochemical reaction is quantitated by LC-MS. |
分子量 | 437.94 |
分子式 | C19H24ClN5O3S |
CAS No. | 886047-22-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 87 mg/mL
Ethanol: 10 mg/mL, Heating is recommended.
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。
LY2119620 886047-22-9 Neuroscience AChR Muscarinic acetylcholine receptor Inhibitor inhibit mAChR LY 2119620 LY-2119620 inhibitor