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Submit ReviewCMPI hydrochloride
说明： Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
化学名： 3-(2-Chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1H-pyrazol-4-yl)isoxazole hydrochloride
纯度： ≥98% (HPLC)
生物活性 for CMPI hydrochloride
CMPI hydrochloride is a potent positive allosteric modulator of α4β2 nAChRs (EC50 values are 20 and 18 nM for rat and human, respectively). Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2(β2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3(β2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.
技术数据 for CMPI hydrochloride
| 分子量 | 379.28 |
| 公式 | C18H19ClN4O.HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2250025-94-4 |
| PubChem ID | 127021040 |
| InChI Key | WNKFVIPYZXTQBR-UHFFFAOYSA-N |
| Smiles | CC1=C(C2=CC(C3=C(C=CC=C3)Cl)=NO2)C=NN1C4CCNCC4.Cl |
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 CMPI hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 18.96 | 50 | |
| DMSO | 37.93 | 100 |
制备储备液 for CMPI hydrochloride
以下数据基于产品分子量 379.28。 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 |
|---|---|---|---|
| 1 mM | 2.64 mL | 13.18 mL | 26.37 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.27 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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产品说明书 for CMPI hydrochloride
参考文献 for CMPI hydrochloride
参考文献是支持产品生物活性的出版物。
Hamouda (2016) Photolabeling a nicotinic acetylcholine receptor (nAChR) with an (α4)3(β2)2 nAChR-selective positive allosteric modulator. Mol.Pharmacol. 89 575 PMID: 26976945
Albrecht et al (2008) Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant α4β2 nicotinic acetylcholine receptor potentiators. Bioorg.Med.Chem.Lett. 18 5209 PMID: 18789861
Wang et al (2017) Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J.Biol.Chem. 292 9988 PMID: 28446611
If you know of a relevant reference for CMPI hydrochloride, please let us know.
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关键词: CMPI hydrochloride, CMPI hydrochloride supplier, PAM, positive, allosteric, modulator, Inhibitors, inhibits, CMPI, nAChR, nAChRs, a4b2, alpha4beta2, α4β2, nicotinic, acetylcholine, receptors, photoreactive, Nicotinic, (a4b2), Receptors, (Other, Subtypes), 5963, Tocris Bioscience
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