(±)-Bay K 8644
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50值:作为一种L型Ca2+通道激活剂,EC50值为17.3 nM。
钙通道激活剂可在活化过程中,增加从神经末梢释放的Ach的数量。用作Ca2+通道激活剂,BAY K 8644通常对心脏和平滑肌有正性肌力和血管收缩作用[1]。
体外实验:经证实,在心脏肌细胞和脊髓神经节神经元中,Bay K 8644延长Ca2+通道平均开放时间。使用大鼠心室的实验表明,当终浓度约为1 pM的Bay K 8644加入灌流液中时,Bay K 8644具有较强的正性肌力作用。此外,将Bay K 8644加入到慢性酒精治疗中可显著减少离体海马脑片中戒断的电生理信号[2, 3]。
体内实验:小鼠体内研究表明,Bay K 8644显著改善酒精戒断综合征。当在实验动物体内急性注入Bay K 8644后,可观察到小鼠的惊厥行为延长了2小时。此外,经报道,BAY k 8644也可在内毒素休克的大鼠体内改善低血压。它可以剂量依赖性的方式使内毒素给药的大鼠心率减少37%,使对照组大鼠的心率减少39%[3,4]。
临床试验:到目前为止,还未进行临床试验。
参考文献:
[1]Greenberg DA, Cooper EC and Carpenter C. Calcium channel 'agonist' BAY K 8644 inhibits calcium antagonist binding to brain and PC12 cell membranes. Brain Res. 1987. 305: 3658.
[2]Doledal V and Tucek S. Failure of the calcium channel activator, Bay K 8644, to increase the release of acetylcholine from nerve terminals in brain and diaphragm. Br. J. Pharmac. 1987. 91: 475-9.
[3]Whittington MA, Butterworth AR, Dolin SJ, Patch TL and Little HJ. The effects of chronic treatment with the dihydropyridine, Bay K 8644, on hyperexcitability due to ethanol withdrawal, in vivo and in vitro. Br. J. Pharmacol. 1992. 105: 285-92.
[4] Ives N, King JW, Chernow B and Roth BL. BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. Eur J Pharmacol. 1986. 130: 169-175.
Physical Appearance | Yellow solid |
Storage | Store at -20°C |
M.Wt | 356.3 |
Cas No. | 71145-03-4 |
Formula | C16H15F3N2O4 |
Solubility | ≥36.2 mg/mL in DMSO; ≥11.4 mg/mL in EtOH; insoluble in H2O |
Chemical Name | methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate |
SDF | Download SDF |
Canonical SMILES | CC1=C(C(C(=C(N1)C)[N+](=O)[O-])C2=CC=CC=C2C(F)(F)F)C(=O)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
豚鼠和小牛心肌细胞 |
溶解方法 |
该化合物在乙醇中的溶解度为100 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
280 nM,5分钟 |
应用 |
Bay k 8644增加了豚鼠心房的抽搐紧张,而不改变紧张发展的时间过程。Bay k 8644增加了小腿室肌和浦肯野纤维的动作电位持续时间。Bay k 8644增加了锶电流,改变了通道开放的时间和电压依赖性。 |
动物实验 [2]: | |
动物模型 |
雄性Sprague-Dawley大鼠 |
给药剂量 |
腹腔注射,0.5-4 mg/kg |
应用 |
腹腔给药BAY K 8644(0.5-4 mg/kg)升高心动过缓相关的血压、增加响应于辐射热的尾反应潜伏期、减少运动、诱导肌肉收缩、姿势变化以及减少反射活动。BAY K 8644(4 mg/kg,i.p.)显著增加皮质和纹状体中的高香草酸和3,4-二羟基苯乙酸浓度。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Thomas G, Chung M, Cohen C J. A dihydropyridine (Bay k 8644) that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent[J]. Circulation research, 1985, 56(1): 87-96. [2]. Bourson A, Moser P C, Gower A J, et al. Central and peripheral effects of the dihydropyridine calcium channel activator BAY K 8644 in the rat[J]. European journal of pharmacology, 1989, 160(3): 339-347. |
质量控制和MSDS
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