HJC0197
目录号 : GC17072
A cell-permeable selective inhibitor of Epac1 and Epac2
Cas No.:1383539-73-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2.
Exchange proteins directly activated by cAMP (Epac) are Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP implicated in regulating a wide variety of intracellular processes in response to second messenger cAMP [1].
In vitro: HJC0197 showed an inhibitory effect against Epac2 with an IC50 value of 5.9 μM. In the presence of equal concentration of cAMP, HJC0197 inhibited Epac2 GEF activity to basal levels at 25 μM. HJC0197 also inhibited Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP. HJC0197 was Epac-specific inhibitors that selectively blocked cAMP-induced Epac activation, but didn’t inhibit cAMP-mediated PKA activation. In HEK293/Epac1 and HEK293/Epac2 cells, pretreatment of with 10 μM HJC0197 for 5 min before the administration of 007-AM, a membrane permeable Epac selective agonist, completely blocked Epac1 and Epac2-mediated Akt phosphorylation [2]. In chicken micromass cultures, inhibition of the PKA-independent cAMP-mediators Epac1 and Epac2 with HJC0197 enhanced cartilage formation [3].
References:
[1]. De Rooij J, Zwartkruis F J T, Verheijen M H G, et al. Epac is a Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP[J]. Nature, 1998, 396(6710): 474-477.
[2]. Chen H, Tsalkova T, Mei F C, et al. 5-Cyano-6-oxo-1, 6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP[J]. Bioorganic & medicinal chemistry letters, 2012, 22(12): 4038-4043.
[3]. Juhász T, Matta C, Somogyi C, et al. Mechanical loading stimulates chondrogenesis via the PKA/CREB-Sox9 and PP2A pathways in chicken micromass cultures [J]. Cellular signaling, 2014, 26(3): 468-482.
| Cas No. | 1383539-73-8 | SDF | |
| 化学名 | 4-cyclopentyl-2-[[(2,5-dimethylphenyl)methyl]thio]-1,6-dihydro-6-oxo-5-pyrimidinecarbonitrile | ||
| Canonical SMILES | CC(C=CC(C)=C1)=C1CSC(NC(C2CCCC2)=C3C#N)=NC3=O | ||
| 分子式 | C19H21N3OS | 分子量 | 339.5 |
| 溶解度 | ≤5mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 2.9455 mL | 14.7275 mL | 29.4551 mL |
| 5 mM | 0.5891 mL | 2.9455 mL | 5.891 mL |
| 10 mM | 0.2946 mL | 1.4728 mL | 2.9455 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。