CTPI-2

SKU: orb1219457

Description

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.

Key Properties

• CAS Number: 68003-38-3
• MW: 391.47
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₅N₃O₃
• SMILES: OC(=O)c1ccccc1NS(=O)(=O)c1ccc(Cl)c(c1)[N+]([O-])=O
• Target: SLC25A1
• Solubility: In Vitro: DMSO : 125 mg/mL (350.40 mM)

Bioactivity

• In Vivo:
  CTPI-2 is a unique regulator of glycolysis that limits the metabolic plasticity of cancer stem cells (CSCs). CTPI-2 (26 mg/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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

SLC25A1