8-CPT-2Me-cAMP, sodium salt
(Synonyms: 8-CPT-2MecAMP, 8-pCPTcAMP, 8-pCPT-2′-OMe-cAMP) 目录号 : GC11483
A selective super-activator of Epacs
Cas No.:634207-53-7
Sample solution is provided at 25 µL, 10mM.
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8-CPT-2Me-cAMP, sodium salt is a selective agonist of EPAC [1].
Cyclic AMP guanine nucleotide exchange factors (EPACs) are intracellular sensors for cAMP and function as nucleotide exchange factors for the Ras GTPase homologues Rap1 and Rap2 [1].
8-CPT-2Me-cAMP, sodium salt is a selective EPAC agonist. 8-CPT-2Me-cAMP increased Rap1 activation by EPAC1. Meantime, light chain 2 (LC2) of the microtubule-associated protein MAP1A increased this response. In LC2- and EPAC1-transfected cells, 8-CPT-2Me-cAMP increased cell adhesion to laminin [1]. In Jurkat Tcells, 8-CPT-2Me-cAMP (100 μM) activated Rap1, which was not affected by H-89, a PKA inhibitor [2]. In 1-LN prostate cancer cells, 8-CPT-2Me-cAMP increased Epac1, p-AktS473 and p-AktT308 in a dose-dependent way. 8-CPT-2Me-cAMP increased p-AktS473 and AktS473 kinase activity by two-three fold. Also, 8-CPT-2Me-cAMP activated mTORC1 and mTORC2 [3].
In human prostate cancer cells, 8-CPT-2Me-cAMP increased the levels of p-cPLA2S505, COX-2 and PGE2. However, COX-2, EP4 or mTOR inhibitors inhibited this effect and reduced protein and DNA synthesis induced by Epac1. These results suggested Epac1 was a pro-inflammatory modulator and promoted cell proliferation [4].
References:
[1]. Gupta M, Yarwood SJ. MAP1A light chain 2 interacts with exchange protein activated by cyclic AMP 1 (EPAC1) to enhance Rap1 GTPase activity and cell adhesion. J Biol Chem, 2005, 280(9): 8109-8116.
[2]. Fuld S, Borland G, Yarwood SJ. Elevation of cyclic AMP in Jurkat T-cells provokes distinct transcriptional responses through the protein kinase A (PKA) and exchange protein activated by cyclic AMP (EPAC) pathways. Exp Cell Res, 2005, 309(1): 161-173.
[3]. Misra UK, Pizzo SV. Upregulation of mTORC2 activation by the selective agonist of EPAC, 8-CPT-2Me-cAMP, in prostate cancer cells: assembly of a multiprotein signaling complex. J Cell Biochem, 2012, 113(5): 1488-1500.
[4]. Misra UK, Pizzo SV. Evidence for a pro-proliferative feedback loop in prostate cancer: the role of Epac1 and COX-2-dependent pathways. PLoS One, 2013, 8(4): e63150.
| Cas No. | 634207-53-7 | SDF | |
| 别名 | 8-CPT-2MecAMP, 8-pCPTcAMP, 8-pCPT-2′-OMe-cAMP | ||
| 化学名 | sodium (4aR,6R,7R,7aR)-6-(6-amino-8-((4-chlorophenyl)thio)-9H-purin-9-yl)-7-methoxytetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-2-olate 2-oxide | ||
| Canonical SMILES | CO[C@]([C@]1([H])N2C3=NC=NC(N)=C3N=C2SC4=CC=C(Cl)C=C4)([H])[C@@](O5)([H])[C@@](O1)([H])COP5([O-])=O.[Na+] | ||
| 分子式 | C17H16ClN5O6PS.Na | 分子量 | 507.82 |
| 溶解度 | 0.5mg/mL in ethanol, 25mg/mL in DMSO, 30mg/mL in DMF | 储存条件 | Desiccate 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 | 1.9692 mL | 9.846 mL | 19.692 mL |
| 5 mM | 0.3938 mL | 1.9692 mL | 3.9384 mL |
| 10 mM | 0.1969 mL | 0.9846 mL | 1.9692 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet