EIPA hydrochloride L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride|cas:1345839-28-2|西域试剂

EIPA hydrochloride L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride,99.92%

产品编号：Bellancom-101840A| CAS NO：1345839-28-2| 分子式：C₁₁H₁₉Cl₂N₇O| 分子量：336.22

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-101840A		￥990.00	杭州北京（现货）
Bellancom-101840A		￥1600.00	杭州北京（现货）

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EIPA hydrochloride L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride

产品介绍

EIPA (L593754) hydrochloride 是一种具有口服活性的 TRPP3 通道抑制剂，IC₅₀ 为 10.5 μM。EIPA hydrochloride 可通过抑制 Na⁺/H⁺-exchanger 3 (NHE3) 来促进自噬 (autophagy)。EIPA hydrochloride 也抑制巨胞饮作用 (macropinocytosis)。EIPA hydrochloride 可用于炎症和癌症的研究，如胃癌、结肠癌、胰腺癌。

生物活性

EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma^[5].

体外研究

EIPA hydrochloride (100 μM, 30 min) suppresses TRPP3-mediated Ca²⁺ uptake in X. laevis oocytes.
EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na⁺ current (IC₅₀: 19.5 μM).
EIPA hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na⁺/H⁺-exchanger 3) in IEC-18 cells.
EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells.
EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn²⁺ entry in cerebellar granule neurons^[4].
EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression^[5].
EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein^[7].

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

Cell Proliferation Assay^[5]

Cell Line:	MKN28 cells
Concentration:	5, 10, 25, 50, and 100 μM
Incubation Time:	48 h
Result:	Inhibited cell proliferation in a dose- and time-dependent manner.

Western Blot Analysis

Cell Line:	IEC-18 cells
Concentration:	300 μM
Incubation Time:	6 h
Result:	Increased total LC3-II protein levels and P62 flux. Increased ATG5, 7, 12 and P62 expression.

体内研究
(In Vivo)

EIPA hydrochloride (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice^[6].
EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model^[7].

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

Animal Model:	Male ddY strain mice^[6]
Dosage:	1 mg/kg
Administration:	Intravenous injection
Result:	Attenuated histologic renal damage, and imprved the I/R-induced increases in renal ET-1 contents.

Animal Model:	Air pouch-type LPS-induced inflammation model^[7]
Dosage:	10 mg/kg
Administration:	Oral administration
Result:	Inhibited the LPS-induced infiltration of leukocytes into the pouch. Inhibited the amount of PGE2 in the pouch fluid.

体内研究

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

Animal Model:	Male ddY strain mice^[6]
Dosage:	1 mg/kg
Administration:	Intravenous injection
Result:	Attenuated histologic renal damage, and imprved the I/R-induced increases in renal ET-1 contents.

Animal Model:	Air pouch-type LPS-induced inflammation model^[7]
Dosage:	10 mg/kg
Administration:	Oral administration
Result:	Inhibited the LPS-induced infiltration of leukocytes into the pouch. Inhibited the amount of PGE2 in the pouch fluid.

体内研究

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

Animal Model:	Male ddY strain mice^[6]
Dosage:	1 mg/kg
Administration:	Intravenous injection
Result:	Attenuated histologic renal damage, and imprved the I/R-induced increases in renal ET-1 contents.

Animal Model:	Air pouch-type LPS-induced inflammation model^[7]
Dosage:	10 mg/kg
Administration:	Oral administration
Result:	Inhibited the LPS-induced infiltration of leukocytes into the pouch. Inhibited the amount of PGE2 in the pouch fluid.

性状

Solid

溶解性数据

In Vitro:

DMSO : 130 mg/mL (386.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9742 mL	14.8712 mL	29.7424 mL
5 mM	0.5948 mL	2.9742 mL	5.9485 mL
10 mM	0.2974 mL	1.4871 mL	2.9742 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献