TM-N1324
(Synonyms: Compound 1324, Cpd1324) 目录号 : GC31074
A GPR39 agonist
Cas No.:1144477-35-9
Sample solution is provided at 25 µL, 10mM.
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TM-N1324 is an agonist of G protein-coupled receptor 39 (GPR39).1 It is selective for GPR39 over a panel of 165 GPCRs, including the growth hormone (GH) secretagogue receptor (GHS-R) and motilin receptor, at 1 ?M. TM-N1324 induces inositol phosphate accumulation in HEK293 cells expressing human GPR39 (EC50s = 2 and 201 nM in the presence and absence of zinc, respectively) and cAMP accumulation in COS-7 cells expressing human GPR39 (EC50 = 17 nM in the presence of zinc). It decreases ghrelin secretion and increases somatostatin secretion in isolated mouse gastric mucosa cells when used at a concentration of 1 ?M. TM-N1324 (30 mg/kg) decreases food intake during the dark period and body weight in a mouse model of high-fat diet-induced obesity.2
1.Frimurer, T.M., Mende, F., Graae, A.-S., et al.Model-based discovery of synthetic agonists for the Zn2+-sensing G-protein-coupled receptor 39 (GPR39) reveals novel biological functionsJ. Med. Chem.60(3)886-898(2017) 2.Grunddal, K.V., Diep, T.A., Petersen, N., et al.Selective release of gastrointestinal hormones induced by an orally active GPR39 agonistMol. Metab.49101207(2021)
Cell experiment: | Caco-2 cells are used as an in vitro model of the human intestinal epithelium and permit assessment of the intestinalpermeability of TM-N1324. TM-N1324 is added to either theapical or basolateral side of a confluent monolayer of Caco-2 cells and permeability is measured by monitoring the appearance of the TM-N1324 on the opposite side of the membrane using LC-MS/MS. TM-N1324 (3 µM) is incubated with pooled liver microsomes and incubated at 5 time points over the course of a 45 min experiment finally TM-N1324 is analyzed by LC-MS/MS. The intrinsic clearance (CLint) and t1/2 values for TM-N1324 in humanand mouse microsomes are reported[1]. |
References: [1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898. | |
| Cas No. | 1144477-35-9 | SDF | |
| 别名 | Compound 1324, Cpd1324 | ||
| Canonical SMILES | O=C1CC(C2=CC=C(F)C=C2Cl)C3=C(N(C4=C5N=CNC5=NC=N4)N=C3C)N1 | ||
| 分子式 | C18H13ClFN7O | 分子量 | 397.79 |
| 溶解度 | DMSO : 6 mg/mL (15.08 mM) | 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 | 2.5139 mL | 12.5694 mL | 25.1389 mL |
| 5 mM | 0.5028 mL | 2.5139 mL | 5.0278 mL |
| 10 mM | 0.2514 mL | 1.2569 mL | 2.5139 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet