(±)-Bay K 8644
(Synonyms: 1,4-二氢-2,6-二甲基-5-硝基-4-(2-[三氟甲基]苯基)吡啶-3-羧酸甲酯,SQ 28,873) 目录号 : GC15015
(±)-Bay K 8644是一种二氢吡啶类化合物，作为特异性的L型钙离子通道激动剂，其EC50值为17.3nM
Cas No.:71145-03-4
Sample solution is provided at 25 µL, 10mM.
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(±)-Bay K 8644 is a dihydropyridine compound that acts as a specific agonist of L-type calcium channels, with an EC₅₀ value of 17.3nM[1]. (±)-Bay K 8644 promotes calcium influx into cells by increasing the open time of sarcolemmal calcium channels[2]. (±)-Bay K 8644 is widely used to study the role of L-type calcium channels in cardiovascular function, neurotransmission, and cellular signal transduction mechanisms[3]. (±)-Bay K 8644 has been shown to improve hypotension and regulate heart rate[4].
In vitro, treatment of human liver cancer HepG2 cells with (±)-Bay K 8644 (0.1–100nM) for 3–5 days significantly promoted colony formation and cell proliferation[5]. Under partial depolarization conditions induced by 25mM K⁺, a 5-minute treatment of PC12 cells with (±)-Bay K 8644 (10nM–10μM) enhanced the release of [³H]norepinephrine by 5-fold through calcium channel activation, an effect that was calcium-dependent[6].
In vivo, a single intraperitoneal injection of (±)-Bay K 8644 (1mg/kg) administered 1 hour before testing in an LPS-induced depression model in mice significantly improved depressive-like behaviors, reducing immobility time and increasing activity time[7]. In female Wistar rats, a single intraperitoneal injection of (±)-Bay K 8644 (3–5mg/kg) induced a reversible convulsion-like syndrome within 15 minutes[8].
References:
[1] Bechem M, Schramm M. Calcium-agonists. J Mol Cell Cardiol. 1987 May;19 Suppl 2:63-75.
[2] Wu L, Wang R, Karpinski E, et al. Bay K-8644 in different solvents acts as a transient calcium channel antagonist and a long-lasting calcium channel agonist. J Pharmacol Exp Ther. 1992 Mar;260(3):966-73.
[3] Baydoun AR, Markham A, Morgan RM, et al. Bay K 8644, modifier of calcium transport and energy metabolism in rat heart mitochondria: a new intracellular site of action. Br J Pharmacol. 1990 Sep;101(1):15-20.
[4] Barrús MT, Reviriego J, Marín J. Effect of Ca2+ agonist Bay K 8644 in human placental arteries. Gen Pharmacol. 1995 Sep;26(5):989-96.
[5] Yamaguchi M, Murata T, Ramos JW. The calcium channel agonist Bay K 8644 promotes the growth of human liver cancer HepG2 cells in vitro: suppression with overexpressed regucalcin. Mol Cell Biochem. 2020 Sep;472(1-2):173-185.
[6] Albus U, Habermann E, Ferry DR, et al. Novel 1,4-dihydropyridine (Bay K 8644) facilitates calcium-dependent [3H]noradrenaline release from PC 12 cells. J Neurochem. 1984 Apr;42(4):1186-9.
[7] He E, Ma R, Qu S, et al. L-methionine and the L-type Ca2+ channel agonist BAY K 8644 collaboratively contribute to the reduction of depressive-like behavior in mice. Front Neural Circuits. 2024 Aug 29;18:1435507.
[8] Petersen EN. Bay K 8644 induces a reversible spasticity-like syndrome in rats. Eur J Pharmacol. 1986 Nov 4;130(3):323-6.
(±)-Bay K 8644是一种二氢吡啶类化合物，作为特异性的L型钙离子通道激动剂，其EC50值为17.3nM[1]。(±)-Bay K 8644通过增加肌膜钙离子通道的开放时间，从而促进钙离子内流进入细胞[2]。(±)-Bay K 8644被广泛应用于研究L型钙离子通道在心血管功能、神经传递以及细胞信号转导中的作用机制[3]。(±)-Bay K 8644具有改善低血压和调节心率的功能[4]。
在体外，(±)-Bay K 8644（0.1-100nM）处理人肝癌细胞HepG2细胞3-5天，显著促进细胞集落形成和细胞增殖[5]。(±)-Bay K 8644（10nM-10μM）单独处理PC12细胞处理5分钟，在25mM K⁺诱导的部分去极化条件下，(±)-Bay K 8644通过激活钙通道使[³H]去甲肾上腺素的释放增强5倍，且该效应具有钙依赖性[6]。
在体内，(±)-Bay K 8644（1mg/kg）单次腹腔注射处理LPS诱导的抑郁模型小鼠1小时，(±)-Bay K 8644显著改善小鼠的抑郁行为，减少小鼠的不动时间，并增加活动时间[7]。(±)-Bay K 8644（3-5mg/kg）单次腹腔注射处理雌性Wistar大鼠，15分钟内诱导产生可逆性痉挛样综合征[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells (human liver cancer cell line) |
Preparation Method | HepG2 cells were maintained in Dulbecco's Modification of Eagle's Medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 100μg/ml penicillin, and 100μg/ml streptomycin at 37°C, 5% CO₂. Cells were treated with (±)-Bay K 8644 at various concentrations (0.1-100nM) for 1-5 days. |
Reaction Conditions | 0.1-100nM; 1-5 days |
Applications | (±)-Bay K 8644 (0.1-10nM) significantly promoted colony formation and cell proliferation in HepG2 cells, while higher concentrations (25-100nM) stimulated caspase-3-dependent apoptotic cell death. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Mice received intraperitoneal injections of LPS (1mg/kg) for 7 consecutive days to induce a depression-like model. For intervention, mice were administered (±)-Bay K 8644 (1mg/kg; i.p.) 1 hour before behavioral tests. In combination therapy groups, mice were fed with L-methionine chow (19.5mg/kg) for 7 consecutive days alongside LPS injections. |
Dosage form | 1mg/kg; i.p. |
Applications | (±)-Bay K 8644 administration partially ameliorated LPS-induced depression-like behaviors, reducing immobility time in the forced swim test and increasing central zone activity in the open field test. |
References: | |
| Cas No. | 71145-03-4 | SDF | |
| 别名 | 1,4-二氢-2,6-二甲基-5-硝基-4-(2-[三氟甲基]苯基)吡啶-3-羧酸甲酯,SQ 28,873 | ||
| 化学名 | methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate | ||
| Canonical SMILES | CC1=C(C(C(=C(N1)C)[N+](=O)[O-])C2=CC=CC=C2C(F)(F)F)C(=O)OC | ||
| 分子式 | C16H15F3N2O4 | 分子量 | 356.3 |
| 溶解度 | 50mg/mL in DMSO, 50mg/mL in DMF, 50mg/mL in ethanol | 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 | 2.8066 mL | 14.0331 mL | 28.0662 mL |
| 5 mM | 561.3 μL | 2.8066 mL | 5.6132 mL |
| 10 mM | 280.7 μL | 1.4033 mL | 2.8066 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。
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