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Submit ReviewTM 38837
说明： Highly potent CB1 inverse agonist; peripherally restricted
化学名： 1-(2,4-Dichlorophenyl)-4-ethyl-N-1-piperidinyl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide
纯度： ≥98% (HPLC)
生物活性 for TM 38837
TM 38837 is a highly potent cannabinoid 1 receptor (CB1) inverse agonist (IC50 values are 8.5 nM and 605 nM for inhibition of [3H]-CP 55940 binding at CB1 and CB2 receptors, respectively). Displays 71-fold selectivity for CB1 receptors over CB2 receptors. Inhibits GTP binding to CB1-overexpressing cell membranes in vitro (EC50 = 18.5 nM). Peripherally restricted. Promotes fear behaviors when given by intracerebrovascular (icv) injection in mice.
化合物库 for TM 38837
TM 38837 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for TM 38837
| 分子量 | 617.51 |
| 公式 | C30H25Cl2F3N4OS |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1253641-65-4 |
| PubChem ID | 49779607 |
| InChI Key | VQOCBFYUDSBDCZ-UHFFFAOYSA-N |
| Smiles | CCC1=C(C2=CC=C(C#CC3=CC=C(C(F)(F)F)C=C3)S2)N(C4=C(C=C(C=C4)Cl)Cl)N=C1C(NN5CCCCC5)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for TM 38837
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 12.35 | 20 | |
| ethanol | 12.35 | 20 |
制备储备液 for TM 38837
以下数据基于产品分子量 617.51。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.1 mL | 40.49 mL | 80.97 mL |
| 1 mM | 1.62 mL | 8.1 mL | 16.19 mL |
| 2 mM | 0.81 mL | 4.05 mL | 8.1 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
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产品说明书 for TM 38837
参考文献 for TM 38837
参考文献是支持产品生物活性的出版物。
Hung et al (2010) Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. Chem.Med.Chem. 5 1439 PMID: 20652930
Takano et al (2014) Low brain CB1 receptor occupancy by a second generation CB1 receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: a PET study. Synapse. 68 89 PMID: 24293119
Micale et al (2019) The cannabinoid CB1 antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice. Front.Pharmacol. 10 PMID: 30949045
If you know of a relevant reference for TM 38837, please let us know.
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关键词: TM 38837, TM 38837 supplier, TM38837, cannabinoid, CB1, receptor, inverse, agonist, highly, potent, peripherally, restricted, Receptors, 7131, Tocris Bioscience
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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