| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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| 靶点 |
PKC ( EC50 = 11.7 nM ); NF-κB
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| 体外研究 (In Vitro) |
为了检查 PKC 在 p38MAPK 磷酸化中的作用，使用 PKC 激活剂 Phorbol 12-myristate 13-acetate (PMA) (100 nM) 刺激细胞，该激活剂模拟 PKC 的天然激活剂 DAG 与 PKC 的 C1 区域的结合。在两种细胞类型中观察到PMA对p38MAPK的磷酸化，类似在αT3-1细胞中观察到的GnRH，即缓慢持续激活（30分钟时分别为3.2倍和3.6倍）。PKCs的不同定位可以解释 GnRH 和 PMA 激活的 PKCs 对 p38MAPK 磷酸化中发挥不同作用。一般来说，αT3-1 细胞中 GnRH 和 PMA 刺激 p38MAPK 磷酸化是由电压门控 Ca2+ 通道和 Ca2+ 激发介导的，而在正极化的LβT2 促进性腺激素细胞中，它仅由 Ca2+ 激励诱导[2]。 THP-1 细胞通过 PMA (200 ng/mL；1-5 天) 存在下脓液形成巨噬细胞样细胞 (THP-1巨噬细胞），从而导致形态变化和细胞表面表达增加为特征的巨噬细胞样表型 CD11 和 CD14[3]。 在单核细胞系 THP-1 中，根据死亡、增殖消失、乳胶珠的吞噬作用，PMA 导致比 VD3 更分泌的表型，以及 CD11b 和 CD14 的表达[5]。
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| 体内研究 (In Vivo) |
Phorbol 12-myristate 13-acetate 可用于动物建模，构建湿疹样模型。 Phorbol 12-myristate 13-acetate (PMA) 是一种 PKC 激动剂，可恢复 5-癸酸 (5-HD) 引起的损伤因此，mitoKATP 的激活通过 PKC 保护了 SOD 和 MDA 中的线粒体功能[4]。
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| 细胞实验 |
单层培养的 αT3-1 和 LβT-2 细胞在 37°C、5% CO2 的加湿培养箱中的 DMEM 中生长。当向同一培养基中添加 0.1% FCS 时，血清饥饿持续 16 小时。然后，在指定的时间内，添加 GnRH 和 PMA。 αT3-1 细胞可以使用 jetPRIME 或 ExGen 500 暂时转染，而 LβT2 细胞只能使用 jetPRIME 转染试剂转染。在涉及显性失活 (DN) PKC 的实验中，将 1.5 μg p38α-GFP 或 3 μg DN-PKC 构建体与对照载体 pCDNA3 一起转染至 αT3-1 细胞（在 6 cm 平板中）。使用 4 μg p38α-GFP 与 9 μg DN-PKCs 构建体或对照载体 pCDNA3 组合进行 LβT2 细胞转染（在 10 cm 板中）。转染后约30小时，细胞血清饥饿（0.1% FCS）16小时。然后用 GnRH 或 PMA 刺激，用冰冷的 PBS 洗涤两次，用裂解缓冲液处理，然后进行一个冻融循环。收获细胞后，取上清液进行免疫沉淀实验，并在 4°C 下以 15,000 xg 离心 15 分钟。
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| 动物实验 |
Rats: Male Wistar rats weighing between 250 and 280 grams are used in all experiments. Seven groups of fifteen thirty-five Wistar rats are randomly assigned. (1) A 0.9% normal saline injection is administered to rats in the sham group (n = 21); (2) A 0.9% normal saline injection is administered to rats in the IR group (n = 21) 30 minutes prior to middle cerebral artery occlusion (MCAO); (3) A lateral cerebral ventricle injection of CBX (5 μg/mL×10 μL) is administered to rats in the Carbenoxolone (CBX) group (n = 21) 30 minutes prior to MCAO; (4) Rats in the Sch-6783 group (n = 21) receive a lateral cerebral ventricle injection of DZX (2 mM×30 μL) 30 minutes before MCAO; (5) Rats in the 5-HD group (n = 21) receive a lateral cerebral ventricle injection of 5-HD (100 mM×10 μL); (6) The rats in the DZX + Ro group (n = 15) receive a lateral cerebral ventricle injection of DZX, and after 10 min, Ro-31-8425 (400 μg/kg) is injected 15 minutes before MCAO; (7) Rats in the 5-HD+PMA group (n = 15) receive an intraperitoneal injection of PMA (200 μg/kg) following the injection of 5-HD and DZX.
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| 参考文献 |
| 分子式 |
C36H56O8
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|---|---|
| 分子量 |
616.8251
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| 精确质量 |
616.4
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| 元素分析 |
C, 70.10; H, 9.15; O, 20.75
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| CAS号 |
16561-29-8
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| 外观&性状 |
Solid powder
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| SMILES |
CCCCCCCCCCCCCC(=O)O[C@@H]1[C@H]([C@]2([C@@H](C=C(C[C@]3([C@H]2C=C(C3=O)C)O)CO)[C@H]4[C@@]1(C4(C)C)OC(=O)C)O)C
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| InChi Key |
PHEDXBVPIONUQT-RGYGYFBISA-N
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| InChi Code |
InChI=1S/C36H56O8/c1-7-8-9-10-11-12-13-14-15-16-17-18-29(39)43-32-24(3)35(42)27(30-33(5,6)36(30,32)44-25(4)38)20-26(22-37)21-34(41)28(35)19-23(2)31(34)40/h19-20,24,27-28,30,32,37,41-42H,7-18,21-22H2,1-6H3/t24-,27+,28-,30-,32-,34-,35-,36-/m1/s1
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| 化学名 |
[(1S,2S,6R,10S,11R,13S,14R,15R)-13-acetyloxy-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-14-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] tetradecanoate
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| 别名 |
NSC262244; PD616; NSC 262244; NSC-262244; PD-616; RP-323; PD 616; RP 323; PMA; RP323
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
DMSO: ~100 mg/mL (~162.1 mM)
Ethanol: ~100 mg/mL (~162.1 mM) |
|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.05 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 2.5 mg/mL (4.05 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 5%DMSO + Corn oil: 5.0mg/ml (8.11mM) 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6212 mL | 8.1060 mL | 16.2119 mL | |
| 5 mM | 0.3242 mL | 1.6212 mL | 3.2424 mL | |
| 10 mM | 0.1621 mL | 0.8106 mL | 1.6212 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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