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CAS No.: 76150-91-9

TCPOBOP Catalog No. CSN26384

TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss[1]. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins[2].

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技术信息

生物活性

描述Constitutive androstane receptor (CAR) belonging to the nuclear receptor superfamily plays an important role in the xenobiotic metabolism and disposition^[1]. TCPOBOP is a mCAR agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss (EC50 = 20 nM). TCPOBOP-induced direct hyperplasia has been considered to be CAR-dependent with no evidence of involvement of cytokines or growth factor signaling^[2]. Expression of CYP2B10 and CYP3A11, known CAR target genes, increased 30-fold and 45-fold, respectively, in TCPOBOP-treated mice fed the MCD diet. TCPOBOP treatment reduced hepatic steatosis (44.6 +/- 5.4% vs 30.4 +/- 4.5%, P < 0.05) and serum triglyceride levels (48 +/- 8 vs 20 +/- 1 mg/dL, P < 0.05) in MCD diet-fed mice as compared with the standard diet-fed mice. This reduction in hepatic steatosis was accompanied by an increase in enzymes involved in fatty acid microsomal omega-oxidation and peroxisomal beta-oxidation, namely CYP4A10, LPBE, and 3-ketoacyl-CoA thiolase. The reduction in steatosis was also accompanied by a reduction in liver cell apoptosis and inflammation^[3]. Hepatocyte proliferation induced by TCPOBOP was associated with a stronger proliferative response and earlier S phase entry in c-jun(Δli) mice, compared to WT animals.^[4].
参考文献

[1] Suticha Kittayaruksakul,et al. Activation of constitutive androstane receptor inhibits intestinal CFTR-mediated chloride transport. Biomed Pharmacother. 2019. 111, 1249-1259.
[2] Bharat Bhushan,et al. TCPOBOP-Induced Hepatomegaly and Hepatocyte Proliferation are Attenuated by Combined Disruption of MET and EGFR Signaling. Hepatology. 2019. 69(4), 1702-1718.
[3] Edwina-S Baskin-Bey,et al. Constitutive androstane receptor agonist, TCPOBOP, attenuates steatohepatitis in the methionine choline-deficient diet-fed mouse. World J Gastroenterol. 2007. 13(42), 5635-41.
[4] Vera P Leoni,et al. Expression of c-jun is not mandatory for mouse hepatocyte proliferation induced by two nuclear receptor ligands: TCPOBOP and T3. J Hepatol. 2011. 55(5), 1069-78.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4872 mL
- 12.4360 mL
- 24.8720 mL
- 5 mM
- 0.4974 mL
- 2.4872 mL
- 4.9744 mL
- 10 mM
- 0.2487 mL
- 1.2436 mL
- 2.4872 mL

技术信息

CAS号	76150-91-9	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C16H8Cl4N2O2	运输	蓝冰
分子量	402.06	别名

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