Pimaric Acid是一种大电导钙激活钾通道的调节剂，能增强该通道对电压的敏感性，并稳定KV1.1-KV2.1的开放状态。
Cas No.:127-27-5
Sample solution is provided at 25 µL, 10mM.
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Pimaric Acid is a modulator of the large conductance Ca2+-activated K+ channel, which sensitizes the channel to voltage and stabilizes the open state in KV1.1-KV2.1[1]. Pimaric Acid can induce swelling of both mitochondria and endoplasmic reticulum by activating potassium channels, resulting in mitochondrial cristae becoming diffuse[2]. Pimaric Acid can be used to disrupt the plasma membrane of bacteria and inhibit the growth of Paenibacillus larvae [3].
In vitro, Pimaric Acid treatment for 24 hours significantly inhibited the production of NO in BV-2 cells under lipopolysaccharide (LPS) stress, with an IC50 value of 13.6μM[4]. Treatment with 20μM of Pimaric Acid for 48 hours significantly inhibited the viability of PA-1 cells and altered the morphology, promoting the upregulation of endoplasmic reticulum stress-related proteins, including p-PERK, PERK, AT-4, CHOP and IRE-1[5]. Treatment with 20μM of Pimaric Acid for 24 hours reduced the MMP-9 protein level in human aortic smooth muscle cells (HASMC) stimulated by TNF-α, accompanied by decreased expressions of p65, c-Fos, p-c-Jun, p-ATF2, and Jun-D, and inhibition of cell migration[6].
References:
[1] Sakamoto K, Suzuki Y, Yamamura H, et al. Molecular mechanisms underlying pimaric acid-induced modulation of voltage-gated K+ channels[J]. Journal of Pharmacological Sciences, 2017, 133(4): 223-231.
[2] Hoa N, Myers M P, Douglass T G, et al. Molecular mechanisms of paraptosis induction: implications for a non-genetically modified tumor vaccine[J]. PloS one, 2009, 4(2): e4631.
[3] Song H, Kim J, Shin Y K, et al. Antibacterial activity of pimaric acid against the causative agent of American foulbrood, Paenibacillus larvae[J]. Journal of Apicultural Research, 2022, 61(2): 219-226.
[4] Kim C S, Oh J, Subedi L, et al. Structural characterization of terpenoids from Abies holophylla using computational and statistical methods and their biological activities[J]. Journal of natural products, 2018, 81(8): 1795-1802.
[5] Li W, Xuemei G, Yilin Z, et al. Anticancer effects of Pimaric acid is mediated via endoplasmic reticulum stress, caspase-dependent apoptosis, cell cycle arrest, and inhibition of cell migration in human ovarian cancer cells[J]. Acta Biochimica Polonica, 2022, 69(1): 245-250.
[6] Suh S J, Kwak C H, Chung T W, et al. Pimaric acid from Aralia cordata has an inhibitory effect on TNF-α-induced MMP-9 production and HASMC migration via down-regulated NF-κB and AP-1[J]. Chemico-Biological Interactions, 2012, 199(2): 112-119.
Pimaric Acid是一种大电导钙激活钾通道的调节剂，能增强该通道对电压的敏感性，并稳定KV1.1-KV2.1的开放状态[1]。Pimaric Acid可通过激活钾通道诱导线粒体和内质网肿胀，导致线粒体嵴变得弥散[2]。Pimaric Acid可用于破坏细菌的质膜并抑制Paenibacillus larvae的生长[3]。
在体外，Pimaric Acid处理24小时显著抑制了脂多糖（LPS）应激下BV-2细胞中一氧化氮的产生，其IC50值为13.6µM[4]。使用20µM的Pimaric Acid处理48小时，显著抑制了PA-1细胞的活力并改变了细胞形态，促进了内质网应激相关蛋白的上调，包括p-PERK、PERK、ATF-4、CHOP和IRE-1[5]。使用20µM的Pimaric Acid处理24小时，降低了TNF-α刺激的人主动脉平滑肌细胞（HASMCs）中MMP-9蛋白水平，同时伴有p65、c-Fos、p-c-Jun、p-ATF2和Jun-D表达的下降，并抑制了细胞迁移[6]。
| Cell experiment [1]: | |
Cell lines | PA-1 cells |
Preparation Method | PA-1 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). PA-1 cells (1×103) were plated using 96-well plates and subjected to incubation for 12h in a 5% CO2 incubator. Incubation was followed by treatment with different doses of Pimaric Acid (0, 2.5, 5, 10, 20, 40, 80, 160, and 320μM) for 48h, and cell viability was measured. |
Reaction Conditions | 0, 2.5, 5, 10, 20, 40, 80, 160 and 320μM; 48h |
Applications | Pimaric Acid treatment decreased the cell viability of PA-1 cells in a dose of manner. |
References: | |
| Cas No. | 127-27-5 | SDF | |
| 别名 | 海松酸 | ||
| Canonical SMILES | C=C[C@@]1(C)C=C2CC[C@@]3([H])[C@@](C(O)=O)(C)CCC[C@]3(C)[C@@]2([H])CC1 | ||
| 分子式 | C20H30O2 | 分子量 | 302.5 |
| 溶解度 | DMSO : 100 mg/mL (330.63 mM; Need ultrasonic) | 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 | 3.3058 mL | 16.5289 mL | 33.0579 mL |
| 5 mM | 661.2 μL | 3.3058 mL | 6.6116 mL |
| 10 mM | 330.6 μL | 1.6529 mL | 3.3058 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
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