CE3F4|cas:143703-25-7|西域试剂

CE3F4,98.39%

产品编号：Bellancom-108539| CAS NO：143703-25-7| 分子式：C₁₁H₁₀Br₂FNO| 分子量：351.01

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货号	价格	库存与货期
Bellancom-108539	￥600.00	杭州北京（现货）
Bellancom-108539	￥1000.00	杭州北京（现货）
Bellancom-108539	￥3500.00	杭州北京（现货）
Bellancom-108539	￥5600.00	杭州北京（现货）

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CE3F4

产品介绍

CE3F4 是一种选择性的 Epac1 拮抗剂，对 Epac1 和 Epac2(B) 的 IC₅₀ 值分别为 10.7 μM 和 66 μM。

生物活性

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC₅₀s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

体外研究

CE3F4 is a selective antagonist of Epac1, with IC₅₀s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC₅₀, 56 μM), but less active than (R)-CE3F4 (IC₅₀, 5.8 μM). CE3F4 (50 μM) shows more inhibitory activities against GEF activity of Epac1, than that of Epac2(AB) or Epac2(B). CE3F4 reduces the exchange activity of Epac1 induced by 007, with IC₅₀ of 23 ± 3 μM. CE3F4 (40 μM) specifically inhibits Epac1 guanine nucleotide exchange activity without interference with Rap1 activity or Epac1-Rap1 interaction. CE3F4 has no influence on PKA activity. CE3F4 (20 μM) inhibits Epac-induced Rap1 activation in living cultured HEK293 cells. CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

CE3F4 (1-3 mg/kg; through a catheter in the internal jugular vein) inhibits atrial fibrillation (AF) and CE3F4 (3 mg/kg; i.v.) inhibits ventricular arrhythmias^[4].
CE3F4 (10 mg/kg; i.v.) improves cardiac function after myocardial infarction in mice^[5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild-type (WT) mice (induced AF after 20min of CE3F4 administration)^[4]
Dosage:	3 mg/kg and 1mg/kg
Administration:	Through a catheter in the internal jugular vein
Result:	Shortened the duration of the pacing-induced AF at 3mg/kg.

Animal Model:	Casq2-KO mice (premature ventricular contraction induced by isoproterenol injection 20min after CE3F4 administration)^[4]
Dosage:	3 mg/kg
Administration:	I.v.
Result:	Reduced the incidence of sympathetic activation-induced ventricular arrhythmias.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild-type (WT) mice (induced AF after 20min of CE3F4 administration)^[4]
Dosage:	3 mg/kg and 1mg/kg
Administration:	Through a catheter in the internal jugular vein
Result:	Shortened the duration of the pacing-induced AF at 3mg/kg.

Animal Model:	Casq2-KO mice (premature ventricular contraction induced by isoproterenol injection 20min after CE3F4 administration)^[4]
Dosage:	3 mg/kg
Administration:	I.v.
Result:	Reduced the incidence of sympathetic activation-induced ventricular arrhythmias.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (142.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8489 mL	14.2446 mL	28.4892 mL
5 mM	0.5698 mL	2.8489 mL	5.6978 mL
10 mM	0.2849 mL	1.4245 mL	2.8489 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。