2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPM2-IN-2

TRPM2-IN-2 是一种高效且选择性的 TRPM2 抑制剂 (IC50 = 0.66 μM)，对 TRPM8 和 TRPV1 的活性极低 (IC50 > 10 μM)。TRPM2-IN-2 在体外氧糖剥夺/再灌注 (OGD/R) 模型和体内短暂性大脑中动脉阻塞 (tMCAO) 小鼠模型中均表现出显著的神经保护作用。TRPM2-IN-2 可用于缺血性卒中的相关研究。

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TRPM2-IN-2

TRPM2-IN-2 Chemical Structure

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TRPM2-IN-2 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

查看所有亚型
TRPA1 TRPC3 TRPC4 TRPC5 TRPM8 TRPM2 TRPM3 TRPM4 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC50 = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC50 >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research[1].

IC50 & Target[1]

TRPM2

0.66 μM (IC50)

体外研究
(In Vitro)

TRPM2-IN-2 (LC4) (0.03-10 μM, 6-24 小时) 在 OGD/R 细胞模型中显示出金刚烷衍生物的保护作用，且对 SH-SY5Y 细胞的细胞毒性较低[1]。
TRPM2-IN-2 (10 μM) 对 TRPV1 和 TRPM8 的抑制活性较低，抑制率分别为 20.5% 和 23.2%[1]。
TRPM2-IN-2 对 CHO 细胞中 hERG 通道的抑制 IC50 为 21.61 μM[1]。

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

TRPM2-IN-2 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 6 and 24 h
Result: Showed low cytotoxicity in SH-SY5Y cells at 10 μM.
Showed no significant cytotoxicity in SH-SY5Y cells up to 1 μM.
Exhibited significant protective effects against OGD/R-induced injury at 0.1 μM and notably maintaining protection even at 0.03 μM.
Did not exhibit significant cytotoxicity at its effective concentration (0.03-0.3 μM).
体内研究
(In Vivo)

TRPM2-IN-2 (0.3、1 和 3 mg/kg，静脉注射，单次给药，灌注后 3 小时) 在 tMCAO 小鼠模型中显示出显著的神经保护作用[1]。

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

Animal Model: Male C57BL/6J mice (8-10 weeks) subjected to 1 h of ischemia followed by 3 h of reperfusion[1]
Dosage: 0.3, 1 and 3 mg/kg
Administration: i.v., single dose at 3 h post-reperfusion
Result: Significantly reduced infarct volume (35.7 %) compared with the vehicle group (60.9 %) at 3 mg/kg.
Exhibited comparable efficacy to 3 mg/kg of Edaravone (HY-B0099) at 1 mg/kg.
Did not show significant protection at 0.3 mg/kg.
Had significantly better outcomes than the vehicle at 3 mg/kg.
Showed no significant improvement compared with vehicle at 0.3 and 1 mg/kg.
significantly lowered levels of MDA (6.8 μM/mgprot) and LDH (0.18 U/mgprot).
分子量

391.51

Formula

C24H29N3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TRPM2-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRPM2-IN-2TRP ChannelTransient receptor potential channelsTRPM2neuroprotectiveOGD/RtMCAOischemic strokeInhibitorinhibitorinhibit

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