2. Membrane Transporter/Ion Channel GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis
  3. TRP Channel Cannabinoid Receptor Interleukin Related TNF Receptor
  4. TRPM8 antagonist 4

TRPM8 antagonist 4 是具有高的功能选择性和良好的理化性质的 CB2R 部分激动剂 (EC50=54.2 μM, Ki=3.2 μM) 和 TRPM8 (IC50=42.3 nM) 拮抗剂。TRPM8 antagonist 4 具有显著的抗炎和镇痛功效以及良好的安全性，降低 TNF-α、IL-6 和 IL-1β 的 mRNA 表达。

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TRPM8 antagonist 4 Chemical Structure

TRPM8 antagonist 4 Chemical Structure

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TRPM8 antagonist 4 相关抗体

Top Publications Citing Use of Products

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TRPC TRPM TRPV TRPA TRPML

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CB1 CB2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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TNFRSF1A/CD120a TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPM8 antagonist 4 is a CB2R partial agonist (EC50=54.2 nM, Ki=3.2 μM) and TRPM8 antagonists (IC50=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β[1].

IC50 & Target

TRPM8

42.3 nM (IC50)

CB2R

54.2 nM (EC50)

CB2R

3.2 μM (Ki)

IL-6

 

IL-1β

 

TNF-α

 

体外研究
(In Vitro)

TRPM8 antagonist 4 (Compound 6b) 在 HTRF cAMP 测定中对 CB1R 既无拮抗活性，亦无激动活性[1]。

TRPM8 antagonist 4 (1 nM-1000 nM) 可抑制 30.0 μM薄荷醇在 HEK293 细胞中诱导的 hTRPM8 电流，IC50=42.3 nM[1]。

TRPM8 antagonist 4 (1 μM -1 M) 通过放射性配体竞争测定，可与 CB2R 结合 [1]。

TRPM8 antagonist 4 (0.3 μM，8 小时) 可降低 LPS 刺激的 RAW264.7 巨噬细胞中 TNF-α、 IL-6 和 IL-1β 的 mRNA 表达[1]。

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

TRPM8 antagonist 4 相关抗体:

RT-PCR[1]

Cell Line: LPS(HY-D1056)-stimulated(100 ng/mL, 8 h) RAW264.7 macrophages
Concentration: 0.3 μM
Incubation Time: 8h
Result: Reduced the mRNA expression of TNF-α, IL-6, and IL-1β compared to LPS-induced model group.
Were comparable to those of CBG at the same concentration the inhibitory effects of on pro-inflammatory cytokine mRNA expression.
体内研究
(In Vivo)

TRPM8 拮抗剂 4 (Compound 6b) (2.5 mg/kg，腹腔注射，一次) 在脂多糖诱导的炎症C57BL/6J 小鼠中表现出抗炎作用[1]。

TRPM8 拮抗剂 4 (5 mg/kg，腹腔注射，一次) 在乙酸诱导 C57BL/6J 小鼠中表现出镇痛作用[1]。

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

Animal Model: LPS (HY-D1056)-induced(i.p., 0.5 mg/kg) inflammation in C57BL/6J mice[1]
Dosage: 2.5 mg/kg
Administration: i.p., once
Result: Suppressed LPS-induced increases in serum IL-6, TNF-α levels.
Animal Model: The Acetic acid-induced (i.p., of 1% acetic acid, 10 mL/kg) in C57BL/6J mice[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: i.p., once
Result: Reduced the number of writhing, prolonged the latency to the first writhing at a concentration of 5 mg/kg.
分子量

329.43

Formula

C20H27NO3
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

TRPM8 antagonist 4 相关分类

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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:

TRPM8 antagonist 4TRP ChannelCannabinoid ReceptorInterleukin RelatedTNF ReceptorTransient receptor potential channelsILTumor Necrosis Factor ReceptorTNFRInflammatory diseasesagonistantagonistHEK293 cellsRAW264.7 macrophagesAnalgesicAnti-inflammatoryInhibitorinhibitorinhibit

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