EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB 2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.
性状
Solid
IC50 & Target[1][2]
PPARγ CB2
体内研究(In Vivo)
EHP-101 (VCE-004.8; i.p.; 20?mg/kg/day; for 3 weeks) induces a significant reduction in body weight gain, total fat mass, adipocyte volume and plasma triglycerides levels in HFD mice. VCE-004.8 can also significantly ameliorate glucose tolerance, reduce leptin levels (a marker of adiposity) and increase adiponectin and incretins (GLP-1 and GIP) levels. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Navarrete C, et al. Hypoxia mimetic activity of VCE-004.8, a cannabidiol quinone derivative: implications for multiple sclerosis therapy. J Neuroinflammation. 2018 Mar 1;15(1):64.[2]. Palomares B, et al. VCE-004.8, A Multitarget Cannabinoquinone, Attenuates Adipogenesis and Prevents Diet-Induced Obesity. Sci Rep. 2018 Oct 31;8(1):16092.
溶解度数据
In Vitro: DMSO : 50 mg/mL (115.32 mM; Need ultrasonic)配制储备液