2. GPCR/G Protein TGF-beta/Smad Metabolic Enzyme/Protease
  3. G protein-coupled Bile Acid Receptor 1 TGF-β Receptor MMP
  4. LIFR/GPBAR1 modulator 1

LIFR/GPBAR1 modulator 1是一种口服有效的，强效 GPBAR1 激动剂 (EC50 = 0.2 μM) 和 LIFR 抑制剂 (IC50 = 7.9 μM)。LIFR/GPBAR1 modulator 1 可上调白血病抑制因子 (LIF) 介导的 LIFR 和 GPBAR1 mRNA 表达，并显著降低促纤维化标志物 (COL1A1、ASMA 和 TGFβ) 的表达，同时降低 TIMP1 表达并增加 MMP9 表达。LIFR/GPBAR1 modulator 1可用于研究人类纤维化疾病。

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LIFR/GPBAR1 modulator 1

LIFR/GPBAR1 modulator 1 Chemical Structure

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LIFR/GPBAR1 modulator 1 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM). LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF)-mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders[1].

IC50 & Target

MMP9

 

体外研究
(In Vitro)

LIFR/GPBAR1 modulator 1 (Compound 2o) (0.1-50 μM) 在 HepG2 细胞中，浓度为 10 μM 时对 LIFR 的抑制率为 89.6 % (IC50 = 7.9 μM)。在 HEK293T 细胞中，浓度为 10 μM 时对 GPBAR1 的激活率为 79.4 % (EC50 = 0.2 μM)[1]。
LIFR/GPBAR1调节剂1 (1–10 μM，24 h) 以浓度依赖的方式调节白血病抑制因子 (LIF) 介导的人肝星状细胞 (HSC) LX2 中纤维化相关基因的表达。在 10 μM 浓度下，它上调 LIFR 和 GPBAR1 的 mRNA 表达，并显著降低促纤维化标志物 (COL1A1、ASMA和TGFβ) 的表达。同时，它降低 TIMP1 的表达并增加 MMP9 的表达，表明其促进细胞外基质 (ECM) 降解[1]。

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

LIFR/GPBAR1 modulator 1 相关抗体:

Real Time qPCR[1]

Cell Line: Leukaemia inhibitory factor (LIF)-mediated human HSC LX2
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Upregulated the mRNA expression of LIFR and GPBAR1 and significantly reduced the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ).
Reduced TIMP1 expression and increased MMP9 expression.
体内研究
(In Vivo)

LIFR/GPBAR1 modulator 1 (Compound 2o) (10 mg/kg，口服，每日一次，持续 7 天) 可有效逆转 Carbon tetrachloride (HY-Y0298) (CCl4) 诱导的小鼠急性肝纤维化，具体表现为减少肝细胞损伤、抑制炎症反应、减少细胞外基质 (ECM) 沉积以及下调促纤维化基因的表达[1]。

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

Animal Model: Liver fibrosis was induced by intraperitoneal (i.p.) administration of carbon tetrachloride (CCl4) at a dose of 500 μL/kg, dissolved in an equal volume of olive oil, and administered twice per week for 1 week to Male C57BL/6J mice[1].
Dosage: 10 mg/kg
Administration: P.o., once daily for 7 days
Result: Reduced weight loss.
Significantly reduced plasma levels of AST, ALT, bilirubin, and LDH.
Reduced CCl4-induced white blood cell (WBC) count elevation and modulated the percentages of neutrophils, lymphocytes, and monocytes.
Improved hepatocellular necrosis and inflammatory infiltration and significantly reduced collagen deposition and fibrosis area.
Significantly downregulated the mRNA expression of fibrosis marker genes (Colla1, aSma, Tgβ) in liver tissue.
分子量

461.59

Formula

C32H31NO2
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

LIFR/GPBAR1 modulator 1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

LIFR/GPBAR1 modulator 1G protein-coupled Bile Acid Receptor 1TGF-β ReceptorMMPG-protein coupled receptor 19GPCR19TGR5GPBAR1Transforming growth factor beta receptorsMatrix metalloproteinasesLIFRLiver fibrosisHepatic stellate cellsHSCInhibitorinhibitorinhibit

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