MCHr1 antagonist 2
目录号 : GC31505
MCHr1antagonist2是一种黑色素聚集激素受体1(melaninconcentratinghormonereceptor1)拮抗剂，IC50值为65nM；MCHr1antagonist2同时抑制hERG，在IMR-32细胞中，IC50值为4.0nM。
Cas No.:863115-70-2
Sample solution is provided at 25 µL, 10mM.
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MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
MCHr1 antagonist 2 (Compound 30) is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM. MCHr1 antagonist 2 has inhibitory effects on Ca2+ flux, and hERG, with IC50s of 196 ± 30 nM and 4.0 ± 0.8 nM, respectively, in IMR-32 cells[1].
[1]. Lynch JK, et al. Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem. 2006 Nov 2;49(22):6569-84.
Kinase experiment: | In 96-well plates, IMR-32 cells (I3.4.2) membranes (6 μg/well) are incubated in the presence of test compound (MCHr1 antagonist 2) in binding buffer (25 mM HEPES pH 7.4, 1 mM CaCl2, 5 mM MgCl2 and 0.5% BSA) and with 0.05 nM [125I]MCH (2200 Ci/mmol) per well for 60 min at room temperature. Nonspecific binding controls consist of I3.4.2 membranes, 0.05 nM [125I]MCH, and 300 nM human MCH. Total binding controls of I3.4.2 membranes and 0.05 nM [125I]MCH are also included on each plate. The plates are centrifuged for 5 min at 1380 g in a GS-6R desktop centrifuge. The reaction buffer is carefully aspirated from each well without disturbing the pellet. Wash buffer (25 mM HEPES, pH 7.4, 1 mM CaCl2, 5 mM MgCl2, and 0.5 M NaCl) is added to each well and then transferred to a 0.5% polyethylenimine-treated GF/B filtration plate using a plate Filtermate Harvester. The filter plate is washed three times with wash buffer, MicroScint 20 is added to each well, and the plate is read using a Topcount microplate scintillation counter[1]. |
References: [1]. Lynch JK, et al. Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety. J Med Chem. 2006 Nov 2;49(22):6569-84. | |
| Cas No. | 863115-70-2 | SDF | |
| Canonical SMILES | O=C(C1=CC(C2=CC(F)=CC=C2O1)=O)NC3CCN(CC4=CC=C(OCO5)C5=C4)CC3 | ||
| 分子式 | C23H21FN2O5 | 分子量 | 424.42 |
| 溶解度 | DMSO : 10 mg/mL (23.56 mM; ultrasonic and adjust pH to 6 with HCl) | 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 | 2.3562 mL | 11.7808 mL | 23.5616 mL |
| 5 mM | 0.4712 mL | 2.3562 mL | 4.7123 mL |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3562 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。
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet