ESI-08

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ESI-08

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

301177-43-5

ESI-08 是一种有效的选择性EPAC拮抗剂，可以完全抑制EPAC1和EPAC2(IC₅₀为 8.4 μM) 的活性。ESI-08 选择性阻断 cAMP 诱导的EPAC激活，但不抑制 cAMP 介导的 PKA 激活。

生物活性

ESI-08 is a potent and selectiveEPACantagonist, which can completely inhibit bothEPAC1andEPAC2(IC₅₀of 8.4 μM) activity. ESI-08 selectively blocks cAMP-inducedEPACactivation, but does not inhibit cAMP-mediatedPKAactivation^[1].

IC₅₀& Target

IC50: 8.4 μM (EPAC2)^[1]
EPAC1^[1]

体外研究
(In Vitro)

Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely^[1].

分子量

353.48

性状

Solid

Formula

C₂₀H₂₃N₃OS

CAS 号

301177-43-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL(282.90 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.8290 mL	14.1451 mL	28.2901 mL
5 mM	0.5658 mL	2.8290 mL	5.6580 mL
10 mM	0.2829 mL	1.4145 mL	2.8290 mL

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。