Calmidazolium chloride是一种高效的Ca2+钙调蛋白依赖性酶抑制剂，其抑制脑磷酸二酯酶、红细胞Ca2+-ATP酶和磷酸化酶b激酶的IC50值分别为0.01μM、0.2μM和5.0μM。
Cas No.:57265-65-3
Sample solution is provided at 25 µL, 10mM.
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Calmidazolium chloride is a very potent inhibitor of several Ca2+-calmodulin-dependent enzymes, the IC50 values are 0.01μM for brain phosphodiesterase, 0.2μM for erythrocyte Ca2+-ATPase and 5.0μM for phosphorylase b kinase [1]. Calmidazolium chloride is a kind of derivative of the antimycotic miconazole, and proposed as a more specific and useful tool for studying the involvement of calmodulin in biological processes [1].
Calmidazolium chloride (4nM; 1h) inhibited activity of calmodulin (CaM) in Aeromonas hydrophila-induced head kidney macrophage (HKM) [2]. Calmidazolium chloride (5μM) decreased the Ca2+ current in mouse pancreatic β-cells; Calmidazolium chloride (5μM; 10min) stimulated insulin release from mouse pancreatic β-cells [3].
Calmidazolium chloride (3.75µg; i.p.) significantly decreased the level of the phosphodiesterase 1 (PDE1) in damaged muscles of C57BL/6 mice induced by cardiotoxin; Calmidazolium chloride (3.75µg; i.p.) increased the expression of TGF-β2 and IL-10 and down-regulated the mRNA levels of pro-inflammatory TNF-α and IL-6 in CD45+ cells in damaged muscles of C57BL/6 mice induced by cardiotoxin [4].
References:
[1] Van Belle H. R 24 571: A potent inhibitor of calmodulin-activated enzymes [J]. Cell Calcium, 1981, 2(5): 483-494.
[2] Banerjee C, Khatri P, Raman R, et al. Role of calmodulin-calmodulin kinase II, cAMP/protein kinase A and ERK 1/2 on Aeromonas hydrophila-induced apoptosis of head kidney macrophages [J]. PLoS Pathog, 2014, 10(4): e1004018.
[3] Kindmark H, Køohler M, Larsson O, et al. Dissociation between exocytosis and Ca2+-channel activity in mouse pancreatic β-cells stimulated with calmidazolium (compound R 24571) [J]. FEBS letters, 1995, 369(2-3): 315-320.
[4] Hu J, Shi D, Ding M, et al. Calmodulin-dependent signalling pathways are activated and mediate the acute inflammatory response of injured skeletal muscle [J]. The Journal of physiology, 2019, 597(21): 5161-5177.
Calmidazolium chloride是一种高效的Ca2+钙调蛋白依赖性酶抑制剂，其抑制脑磷酸二酯酶、红细胞Ca2+-ATP酶和磷酸化酶b激酶的IC50值分别为0.01μM、0.2μM和5.0μM[1]。Calmidazolium chloride是一种抗真菌药物咪康唑的衍生物，是研究钙调蛋白参与生物过程的一种更特异和有用的工具[1]。
Calmidazolium chloride（4nM；1h）抑制Aeromonas hydrophila感染的HKM（head kidney macrophage）中钙调蛋白的活性[2]。Calmidazolium chloride（5μM）降低小鼠胰岛β细胞中的Ca2+电流；Calmidazolium chloride（5μM；10min）刺激小鼠胰岛β细胞释放胰岛素[3]。
Calmidazolium chloride（3.75µg；i.p.）显著降低心脏毒素诱导的C57BL/6小鼠损伤肌肉中的磷酸二酯酶1的水平；Calmidazolium chloride（3.75µg；i.p.）增加心脏毒素诱导C57BL/6小鼠损伤肌肉中TGF-β2和IL-10的表达，下调促炎因子TNF-α和IL-6 mRNA水平[4]。
| Cell experiment [1]: | |
Cell lines | Head kidney macrophage (HKM) |
Preparation Method | HKM were pre-treated with or without Calmidazolium chloride for 1h, and then HKM were infected with Aeromonas hydrophila for 60min. |
Reaction Conditions | 4nM; 1h |
Applications | Calmidazolium chloride inhibited activity of calmodulin in cells. |
| Animal experiment [2]: | |
Animal models | Male and female C57BL/6 mice |
Preparation Method | The mice in the injury group received cardiotoxin (CTX) injection into the tibialis anterior (TA) muscle and mice in the control group were injected intraperitoneally with an equal volume of saline. Twenty-four hours after the CTX injection, the mice were injected with Calmidazolium chloride. |
Dosage form | 3.75µg (150µl, 25µg/ml) per animal; i.p. |
Applications | Calmidazolium chloride significantly decreased the level of the phosphodiesterase 1 (PDE1) in damaged muscles of mice. |
References: | |
| Cas No. | 57265-65-3 | SDF | |
| 别名 | 钙调蛋白抑制剂,R 24571 | ||
| 化学名 | (S)-1-(bis(4-chlorophenyl)methyl)-3-(2-((2,4-dichlorobenzyl)oxy)-2-(2,4-dichlorophenyl)ethyl)-1H-imidazol-3-ium chloride | ||
| Canonical SMILES | ClC1=CC(Cl)=CC=C1[C@@H](C[N+]2=CN(C=C2)C(C(C=C3)=CC=C3Cl)C(C=C4)=CC=C4Cl)OCC(C(Cl)=C5)=CC=C5Cl.[Cl-] | ||
| 分子式 | C31H23Cl7N2O | 分子量 | 687.7 |
| 溶解度 | 100mM in ethanol, or in DMSO | 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 | 1.4541 mL | 7.2706 mL | 14.5412 mL |
| 5 mM | 290.8 μL | 1.4541 mL | 2.9082 mL |
| 10 mM | 145.4 μL | 727.1 μL | 1.4541 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet