2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Enpp-1-IN-30

Enpp-1-IN-30 (compound 44a) 是一种具有口服生物利用度的 ENPP1 抑制剂，对人源 IC50 为 13.1 nM。Enpp-1-IN-30 可阻止 cGAMP 降解，激活 STING 通路。Enpp-1-IN-30 可诱导细胞因子释放以增强固有免疫应答。Enpp-1-IN-30 在同基因小鼠模型中发挥抗肿瘤功效。Enpp-1-IN-30 可用于结肠癌的研究。

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Enpp-1-IN-30

Enpp-1-IN-30 Chemical Structure

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Customer Review

Enpp-1-IN-30 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Enpp-1-IN-30 (compound 44a) is an orally bioavailable ENPP1 inhibitor with a human IC50 of 13.1 nM. Enpp-1-IN-30 prevents cGAMP degradation, activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance innate immune response. Enpp-1-IN-30 exerts antitumor efficacy in syngeneic mouse models. Enpp-1-IN-30 can be used for the research of colon carcinoma[1].

体外研究
(In Vitro)

Enpp-1-IN-30 (compound 44a) (0.2 nM-1 μM; 2 h) 可强效抑制重组人源 ENPP1，其 IC50 为 13.1 nM[1]。
Enpp-1-IN-30 (up to 10,000 nM) 对 ENPP1 具有高度选择性，在最高 10,000 nM 浓度下对重组人源 ENPP2 或 ENPP3 无可检测到的抑制作用[1]。
Enpp-1-IN-30 (0.01-30 μM; 1 h) 可剂量依赖性增强 HCT116-Dual™ 细胞中 cGAMP 介导的 STING 通路激活，在 10 μM 浓度下使 IRF3 荧光素酶强度提升 8.8 倍，在 30 μM 浓度下提升 10.1 倍[1]。
Enpp-1-IN-30 (10 μM; 1-72 h) 可增强经 cGAMP 共处理的 THP-1 细胞中的固有免疫激活，随时间显著提升 IFNB 和 CXCL10 mRNA 表达，并诱导 TNFA mRNA 表达呈渐进性、非过度性升高[1]。

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

Enpp-1-IN-30 相关抗体:

Real Time qPCR[1]

Cell Line: THP-1 cells
Concentration: 10 μM (co-treated with 10 μM cGAMP)
Incubation Time: 24-72 h (IFNB); 1-72 h (CXCL10, TNFA)
Result: Increased IFNB mRNA expression by 6.7-fold at 72 h (co-treated with 10 μM cGAMP).
Increased CXCL10 mRNA expression by 137-fold at 72 h (co-treated with 10 μM cGAMP).
Induced a gradual increase in TNFA mRNA expression reaching 8-fold at 72 h (co-treated with 10 μM cGAMP), with no instant overexpression of TNFA.
药代动力学
(Parmacokinetics)
Species Dose Route AUClast Cmax Tmax T1/2 Bioavailability CL Vss
Mice[1] 2 mg/kg i.v. 6949 ng·h/mL 3613 ng/mL / 2.42 h / 284 mL/min/kg 658 L/kg
Mice[1] 10 mg/kg p.o. 23464 ng·h/mL 4526 ng/mL 0.5 h 2.97 h 65.8 % / /
体内研究
(In Vivo)

Enpp-1-IN-30 (化合物 44a) (50 mg/kg; p.o.; once daily; 14 days) 可显著降低 MC38 同源结肠癌小鼠模型中的肿瘤体积，与抗 mPD-L1 抗体联合使用时可观察到协同疗效，且无相关毒性[1]。

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

Animal Model: C57BL/6 (7-week-old female)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily; 14 days
Result: Reduced tumor volumes significantly relative to vehicle control group.
Produced synergistic tumor volume reduction in combination with anti-mPD-L1 antibody.
Caused no significant body weight loss or other clinical signs of toxicity.
分子量

349.38

Formula

C15H16FN5O2S
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

Enpp-1-IN-30 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:

Enpp-1-IN-30Phosphodiesterase (PDE)THP-1 cellscGAMPinnate immune responseSTING pathwaysyngeneic mouse modelsENPP2colon carcinomaENPP3ENPP1HCT116-Dual? cellsInhibitorinhibitorinhibit

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