CTPI-2 是第三代特异性线粒体柠檬酸盐载体 SLC25A1 抑制剂，K_D 为 3.5 μM。CTPI-2 抑制糖酵解、PPARγ 及其下游靶点葡萄糖转运蛋白 GLUT4。CTPI-2 阻断非酒精性脂肪性肝炎逆转脂肪变性的显著改变，防止演变为脂肪性肝炎，减少肝脏和脂肪组织中炎性巨噬细胞的浸润，并显著减轻由高脂肪饮食引起的肥胖。具有抗肿瘤活性。

CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a K D of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. 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. Antitumor activity.

Solid

KD: 3.5 μM (SLC25A1)

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. has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Tan M, et al. Inhibition of the mitochondrial citrate carrier, Slc25a1, reverts steatosis, glucose intolerance, and inflammation in preclinical models of NAFLD/NASH. Cell Death Differ. 2020;27(7):2143-2157.
[2]. Fernandez HR, et al. The mitochondrial citrate carrier, SLC25A1, drives stemness and therapy resistance in non-small cell lung cancer. Cell Death Differ. 2018;25(7):1239-1258.

In Vitro: DMSO : 125 mg/mL (350.40 mM; Need ultrasonic)配制储备液