CTPI-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CTPI-2 是线粒体柠檬酸载体 SLC25A1 的抑制剂，KD ：3.5 μM。 CTPI-2 抑制糖酵解 PPARγ 及其下游目标葡萄糖转运蛋白 GLUT4。

CTPI-2 is an inhibitor of mitochondrial citrate carrier SLC25A1 with(KD : 3.5 μM).?CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4.?CTPI-2 exhibits anti-tumor activity.CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet.CTPI-2, halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, while starkly mitigating obesity induced by a high-fat diet.?These effects are differentially recapitulated by a global ablation of one copy of the Slc25a1 gene or by a liver-targeted Slc25a1 knockout, which unravel dose-dependent and tissue-specific functions of this protein.?Mechanistically, through citrate-dependent activities, Slc25a1 inhibition rewires the lipogenic program, blunts signaling from peroxisome proliferator-activated receptor gamma, a key regulator of glucose and lipid metabolism, and inhibits the expression of gluconeogenic genes.?The combination of these activities leads not only to inhibition of lipid anabolic processes, but also to a normalization of hyperglycemia and glucose intolerance as well.

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CTPI-2 is a unique regulator of glycolysis that limits the metabolic plasticity of cancer stem cells (CSCs). CTPI-2 (26mg/kg; i.p.) inhibits tumor growth in in vivo models of non-small cell lung cancer (NSCLC).CTPI-2 (50 mg/kg; i.p.; alternate days for 12 weeks) completely averts weight gain in the prevention study and leads to significant weight loss in the reversion study.?CTPI-2 prevents steatohepatitis and normalizes glucose tolerance. CTPI-2 lowers the levels of circulating IL-6 while increasing anti-inflammatory IL-4 and IL-10 and also reduced the monocyte chemoattractant protein-1 and monokine-induced by interferon-γ that attract neutrophils and monocytes. CTPI-2 regulates the citrate pool, the lipogenic and the gluconeogenic pathways. Animal Model:C57BL/6J mice (HFD-fed mice) Dosage:50 mg/kg Administration:Alternate days via the intraperitoneal route for 12 weeks Result:Completely averted weight gain in the prevention study and led to significant weight loss in the reversion study.

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Others

Other Targets

SLC25A1

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68003-38-3

391.47

C23H25N3O3

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (350.40 mM)

OC(=O)c1ccccc1NS(=O)(=O)c1ccc(Cl)c(c1)[N+]([O-])=O

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(-20℃)

With Ice Pack

≥ 2 years