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Submit ReviewMibefradil dihydrochloride
说明： CaV3.x blocker
别名： Ro 40-5967
化学名： (1S,2S)-2-[2-[[3-(1H-Benzimidazol-2yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl methoxyacetoacetate dihydrochloride
纯度： ≥97% (HPLC)
生物活性 for Mibefradil dihydrochloride
Mibefradil dihydrochloride is a Ca2+ channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 μM and 18.6 μM for T-type and L-type channels respectively. Antihypertensive agent.
化合物库 for Mibefradil dihydrochloride
Mibefradil dihydrochloride 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 Mibefradil dihydrochloride
| 分子量 | 568.56 |
| 公式 | C29H38FN3O3.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 116666-63-8 |
| PubChem ID | 60662 |
| InChI Key | MTJLQTFHJIHXIX-GDUXWEAWSA-N |
| Smiles | Cl.Cl.COCC(=O)O[C@]1(CCN(C)CCCC2=NC3=C(N2)C=CC=C3)CCC2=C(C=CC(F)=C2)[C@@H]1C(C)C |
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 Mibefradil dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 28.43 | 50 | |
| DMSO | 56.86 | 100 |
制备储备液 for Mibefradil dihydrochloride
以下数据基于产品分子量 568.56。 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 | 1.76 mL | 8.79 mL | 17.59 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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产品说明书 for Mibefradil dihydrochloride
参考文献 for Mibefradil dihydrochloride
参考文献是支持产品生物活性的出版物。
Osterrieder and Holck (1989) In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action. J.Cardiovasc.Pharmacol. 13 754 PMID: 2472524
Veniant et al (1991) Hemodynamic profile of Ro 40-5967 in conscious rats: comparison with diltiazem, verapamil, and amlod. J.Cardiovasc.Pharmacol. 18 S55 PMID: 1725005
Mehrke et al (1994) The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J.Pharmacol.Exp.Ther. 271 1483 PMID: 7996461
If you know of a relevant reference for Mibefradil dihydrochloride, please let us know.
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关键词: Mibefradil dihydrochloride, Mibefradil dihydrochloride supplier, Ca2+, channel, blockers, T-type, Calcium, CaV, Channels, L-Type, P-Type, R-Type, Q-Type, T-Type, N-Type, voltage-gated, voltage-dependent, Ro405967, Ro, 40-5967, Cav3.x, 2198, Tocris Bioscience
9 篇 Mibefradil dihydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Mibefradil dihydrochloride 的部分引用包括：
Higley and Sabatini (2010) Competitive regulation of synaptic Ca2+ influx by D2 DA and A2A adenosine receptors. Nat Neurosci 13 958 PMID: 20601948
Wang et al (2015) Hydrogen sulfide-induced itch requires activation of Cav3.2 T-type calcium channel in mice. Nature 5 16768 PMID: 26602811
Prigge et al (2016) M1 ipRGCs Influence Visual Function through Retrograde Signaling in the Retina The Journal of Neuroscience 6 7184 PMID: 27383593
Weick and Demb (2011) Delayed-rectifier K channels contribute to contrast adaptation in mammalian retinal ganglion cells. Neuron 71 166 PMID: 21745646
Weber (2017) Activation of odorant receptor in colorectal cancer cells leads to inhibition of cell proliferation and apoptosis. PLoS One 12 e0172491 PMID: 28273117
Grubb and Burrone (2010) Activity-dependent relocation of the axon initial segment fine-tunes neuronal excitability. Neurosci Lett 465 1070 PMID: 20543823
Bragança et al (2016) Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol 7 45 PMID: 27014060
Stone et al (2013) Attenuation of autonomic reflexes by A803467 may not be solely caused by blockade of NaV 1.8 channels. Sci Rep 543 177 PMID: 23523647
Cilz et al (2014) DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
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Mibefradil dihydrochloride used on T type calcium channels.
By
Anonymous on 02/13/2019
种属： Human
Mibefradil dihydrochloride used on T type calcium channels that aid in mediating calcium influx into cells after an action potential or depolarizing signal. The entry of calcium into various cells has many different physiological responses associated with it.
