VCE-004.8 (VCE-004.8) 是一种具有口服活性的特异性 PPARγ;和 CB2 受体双重激动剂。
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VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity[1]. VCE-004.8 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. VCE-004.8 attenuates adipogenesis and prevents diet-induced obesity[2]. PPARγ CB2
VCE-004.8 ( injection; 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[1].
[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.
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