2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB Apoptosis
  3. Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related
  4. PDE/TRPA1/CHIT1-IN-1

PDE/TRPA1/CHIT1-IN-1 是一种 PDEs、TRPA1 及 hCHIT1 (KD 值为 37.7 μM) 抑制剂。 PDE/TRPA1/CHIT1-IN-1 是一种广谱 PDE 抑制剂，可强效作用于包括 PDE4B、PDE7A、PDE3A 和 PDE8A 在内的关键亚型其 IC50 值分别为 15.54，15.15，8.39 和 16.46 μM。PDE/TRPA1/CHIT1-IN-1 能够抑制 NLRP3 炎症小体激活并阻断 NF-κB 磷酸化，从而下调体内促炎基因 (TNF-α 和 IL-6) 的表达。PDE/TRPA1/CHIT1-IN-1 可用于慢性阻塞性肺疾病及相关炎症性肺病的研究。

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PDE/TRPA1/CHIT1-IN-1

PDE/TRPA1/CHIT1-IN-1 Chemical Structure

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PDE/TRPA1/CHIT1-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

查看 TRP Channel 亚型特异性产品:

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TRPA1 TRPC3 TRPC4 TRPC5 TRPM8 TRPML1 TRPML2 TRPML3 TRPV1 TRPV3 TRPV4

查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
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 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research[1].

IC50 & Target

PDE4B

15.54 μM (IC50)

PDE7A

15.15 μM (IC50)

PDE3A

8.39 μM (IC50)

PDE8A

16.64 μM (IC50)

PDE1B

54.47 μM (IC50)

PDE2A

79.61 μM (IC50)

PDE4D

130.50 μM (IC50)

PDE5A

26.86 μM (IC50)

PDE10A

36.13 μM (IC50)

体外研究
(In Vitro)

PDE/TRPA1/CHIT1-IN-1 (compound 39) (10 μM，1 小时) 在 LPS 刺激的 RAW264.7 巨噬细胞中具有抗炎活性[1]。
PDE/TRPA1/CHIT1-IN-1 抑制 PDE1B、PDE2A、PDE4B、PDE7A、PDE3A、PDE4D、PDE5A、PDE8A 和 PDE10A，其 IC50 值分别为 54.47、79.61、15.54、15.15、8.39、130.50、26.86、16.46 和 36.13 μM[1]。
PDE/TRPA1/CHIT1-IN-1 (1-50 μM，1 小时) 抑制支气管平滑肌细胞增生与肥大，减少 BSMC 和 MRC-5 细胞的细胞外基质成分分泌，并抑制成纤维细胞向肌成纤维细胞的转化[1]。
PDE/TRPA1/CHIT1-IN-1 具有支气管舒张效应，IC50 值为 1.56 μM，并对预收缩的大鼠气管段产生最大舒张率达 100%[1]。
PDE/TRPA1/CHIT1-IN-1 具有高代谢稳定性 (t1/2 = 53.42 分钟，固有清除率 Clint = 32.43 μL/min/mg)、可忽略的肝细胞毒性 (在 HepG2 细胞中 IC50 = 34.70 μM) 和中等的膜渗透性 (logPe = -5.305)[1]。

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

PDE/TRPA1/CHIT1-IN-1 相关抗体:

ELISA Assay[1]

Cell Line: LPS-stimulated RAW264.7 macrophages
Concentration: 10 μM
Incubation Time: 1 h
Result: Caused an almost twofold reduction in TNF-α and IL-6 levels in LPS-induced RAW264.7 cells, lowering TNF-α concentrations to 381.74 pg/mL and decreasing IL-6 concentrations to 141.02 pg/mL.

Cell Proliferation Assay[1]

Cell Line: FBS induced-MRC-5, FBS induced-BSMC, TGF-β (HY-179042) induced- MRC-5 and TGF-β induced-BSMC
Concentration: 1, 10 and 50 μM
Incubation Time: 1 h
Result: Reduced BSMC and MRC-5 proliferation by 38 % and 32 % at a concentration of 10 μM.
Reduced TGF-β-induced expression of COL1A1 and FN1 genes in both cell lines.
Decreased TGF-β-induced ACTA2 expression in BSMCs by almost a 3-fold.
Reduce TGF-β-induced ACTA2 expression in lung fibroblasts.
体内研究
(In Vivo)

PDE/TRPA1/CHIT1-IN-1 (compound 39) (25 mg/kg，腹腔注射，每日一次，持续 2 周) 在弹性蛋白酶诱导的肺气肿模型中显示出抗炎特性并调控 NLRP3 炎症小体[1]。

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

Animal Model: PPE (HY-B2118) (i.n. once a week for 4 week) induced-Balb/c male mice (8-10 weeks, 23-25 kg)[1]
Dosage: 25 mg/kg
Administration: i.p., once daily; for 2 weeks
Result: Protected against elastase-induced emphysema with MLI values of 50.36 μm.
Ameliorated the elastase-induced increase in total inflammatory cells in in bronchoalveolar lavage fluid (BALF).
Reduced the total number of all inflammatory cells in BALF collected from the PPE-induced model.
Acted as a relatively strong inhibitor of PDE7A and PDE3A, as well as a TRPA1 antagonist.
Reduced the PPE-induced transcript levels of key inflammatory genes in lung homogenates to control levels.
Decrease in Tnfa, Cxcl2, Il6, and Il1b expression.
Limited the levels of NLRP3 inflammasome components and consequently reduced the activation of NLRP3 inflammasome components.
Reduced the PPE-induced level of cleaved caspase-1, which may have inhibited the formation of interleukin 1β (IL-1β), a hallmark cytokine of NLRP3 inflammasome activation.
Reduced NF-κB phosphorylation, as well as the expression of various proinflammatory genes, including Tnfa, Cxcl2, Il6, and Il1b.
分子量

547.61

Formula

C28H33N7O5
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

PDE/TRPA1/CHIT1-IN-1 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:

PDE/TRPA1/CHIT1-IN-1Phosphodiesterase (PDE)TRP ChannelNOD-like Receptor (NLR)NF-κBTNF ReceptorInterleukin RelatedTransient receptor potential channelsNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILPDEsTRPA1hCHIT1NLRP3TNF-αIL-6COPDlung diseaseInhibitorinhibitorinhibit

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