Englerin A|cas:1094250-15-3|西域试剂

Englerin A,99.0%

产品编号：Bellancom-133168| CAS NO：1094250-15-3| 分子式：C₂₆H₃₄O₆| 分子量：442.54

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-133168		￥13500.00	杭州北京（现货）

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Englerin A

产品介绍

Englerin A 是一种有效和选择性的 TRPC4 和 TRPC5 通道的活化剂，EC₅₀ 值分别为 11.2 和 7.6 nM。Englerin A 通过增加 Ca²⁺ 内流和 Ca²⁺ 细胞超负荷来诱导肾癌细胞死亡。

生物活性

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca²⁺ influx and Ca²⁺ cell overload.

体外研究

Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs.
Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5.
Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca²⁺ concentration within 1 min in HEK 293 cells over-expressing human TRPC4.
Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca²⁺ elevations in A498 cells as well with an EC₅₀ of 10 nM.

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

体内研究

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice^[4].

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

体内研究

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice^[4].

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

性状

Solid

溶解性数据

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Akbulut Y, et, al. (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91. [Content Brief]

. Rubaiy HN, et, al. Identification of an (-)-englerin A analogue, which antagonizes (-)-englerin A at TRPC1/4/5 channels. Br J Pharmacol. 2018 Mar; 175(5):830-839. [Content Brief]

. Carson C, et, al. Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS One. 2015 Jun 22;10(6):e0127498. [Content Brief]

[4]. Sourbier C, et, al. Englerin A stimulates PKCθ to inhibit insulin signaling and to simultaneously activate HSF1: pharmacologically induced synthetic lethality. Cancer Cell. 2013 Feb 11;23(2):228-37. [Content Brief]

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