2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel NF-κB Immunology/Inflammation
  3. Phosphodiesterase (PDE) TRP Channel NF-κB NOD-like Receptor (NLR) Interleukin Related
  4. Multitarget AD-IN-6

Multitarget AD-IN-6 (Compound 39) 是一种多靶点抑制剂，对人源 PDE4B 的 IC50 为 15.54 μM，对人源 PDE7A 的 IC50 为 15.15 μM，对人源 PDE3A 的 IC50 为 8.39 μM，对人源 CHIT1 的 Kd 为 37.7 μM。Multitarget AD-IN-6 可作为 TRPA1 拮抗剂，降低 NLRP3 炎症小体多蛋白复合物水平以抑制其激活，同时抑制 PDE4B、PDE7A 和 CHIT1，并减少 NF-κB 的磷酸化。Multitarget AD-IN-6 可改善弹性蛋白酶诱导的肺气肿小鼠病理。Multitarget AD-IN-6 可用于慢性阻塞性肺疾病的研究。

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Multitarget AD-IN-6

Multitarget AD-IN-6 Chemical Structure

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Customer Review

Multitarget AD-IN-6 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:

查看所有亚型
TRPA1 TRPC3 TRPC4 TRPC5 TRPM8 TRPM2 TRPM3 TRPM4 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

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

Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC50 of 15.54 μM against human PDE4B, 15.15 μM against human PDE7A, 8.39 μM against human PDE3A, and a Kd of 37.7 μM against human CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease[1].

IC50 & Target[1]

PDE4B

15.54 μM (IC50)

PDE7A

15.15 μM (IC50)

PDE1B

54.47 μM (IC50)

PDE2A

79.61 μM (IC50)

PDE3A

8.39 μM (IC50)

hPDE4D

130.50 μM (IC50)

PDE5A

26.86 μM (IC50)

PDE8A

16.46 μM (IC50)

human PDE 10A

36.13 μM (IC50)

TRPA1

 

IL-6

 

体外研究
(In Vitro)

Multitarget AD-IN-6 可抑制重组人源 PDE4B，其 IC50 为 15.54 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE7A，其 IC50 为 15.15 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE1B，其 IC50 为 54.47 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE2A，其 IC50 为 79.61 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE3A，其 IC50 为 8.39 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE4D，其 IC50 为 130.50 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE5A，其 IC50 为 26.86 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE8A，其 IC50 为 16.46 μM[1]。
Multitarget AD-IN-6 可抑制重组人源 PDE10A，其 IC50 为 36.13 μM[1]。
Multitarget AD-IN-6 (100 μM) 是 TRPA1 通道的拮抗剂，在 100 μM 浓度下可抑制其 51% 的活性，且无激动效应[1]。
Multitarget AD-IN-6 抑制重组人 CHIT1，抑制率为 57%，Kd 值为 37.7 μM[1]。
Multitarget AD-IN-6 (10 μM；1 h) 可抑制 RAW 264.7 小鼠巨噬细胞中 LPS 诱导的一氧化氮、TNF-α 及 IL-6 的产生，展现出抗炎活性[1]。
Multitarget AD-IN-6 (10-50 μM；48 h) 降低胎牛血清 (FBS) 诱导的支气管平滑肌细胞增殖[1]。

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

Multitarget AD-IN-6 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human bronchial smooth muscle cells (BSMC)
Concentration: 10-50 μM
Incubation Time: 48 h
Result: Reduced FBS-induced BSMC proliferation by 38% relative to untreated cells at 10 μM.
Further reduced BSMC proliferation in a concentration-dependent manner at 50 μM.
体内研究
(In Vivo)

Multitarget AD-IN-6 (25 mg/kg；腹腔注射；连续 14 天) 可显著减轻弹性蛋白酶诱导的小鼠 COPD 病理改变，包括气腔扩大、肺部炎症、NLRP3 炎症小体激活及 NF-κB 磷酸化[1]。

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

Animal Model: BALB/c (male, 8-10 weeks old, mean weight 25.5 g, intranasally instilled with porcine pancreatic elastase 4 times weekly for 21 days to induce emphysema)[1]
Dosage: 25 mg/kg
Administration: i.p.; once daily; 14 consecutive days
Result: Reduced mean linear intercept (MLI) from 59.50 μm to 50.36 μm, attenuating elastase-induced air space enlargement.
Significantly reduced the total number of inflammatory cells in BALF in both acute and chronic experimental settings; in the acute model, this effect was stronger than that of roflumilast.
Normalized PPE-induced elevated transcript levels of pro-inflammatory genes *Tnfa*, *Cxcl2*, *Il6*, and *Il1b* in lung homogenates to control levels.
Reduced PPE-induced increases in NLRP3, ASC/TMS1, and cleaved caspase-1 protein levels in lung homogenates to match control levels.
Decreased PPE-induced NF-κB p65 phosphorylation in lung homogenates to control levels.
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

Multitarget AD-IN-6 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)

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

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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:

Multitarget AD-IN-6Phosphodiesterase (PDE)TRP ChannelNF-κBNOD-like Receptor (NLR)Interleukin RelatedTransient receptor potential channelsNuclear factor-κBNuclear factor-kappaBILPDE4Bchronic obstructive pulmonary diseaseTRPA1PDE7Aelastase-induced emphysema murine modelsCHIT1NLRP3 inflammasomehuman airway cell-based modelsRAW 264.7 murine macrophagesInhibitorinhibitorinhibit

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