同义名 :	-
	CAS号 :	76150-91-9
	货号 :	A390654
	分子式 :	C16H8Cl4N2O2
	纯度 :	97%
	分子量 :	402.06
	MDL号 :	MFCD00057368
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.49mL 0.50mL 0.25mL	12.44mL 2.49mL 1.24mL	24.87mL 4.97mL 2.49mL

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.