ucp2

Genipin ((+)-Genipin) 是衍生自黄栀果实的天然交联剂，可抑制细胞中的 UCP2 (解偶联蛋白 2)。它有蛋白质调节、抗肿瘤、抗炎症、免疫抑制、抗血栓形成和对海马神经元保护的多种生物活性，可研究 2 型糖尿病。

Enavermotide (UCP2)是用于主动免疫(抗肿瘤)的免疫制剂。

Darglitazone (CP-86325) 是一种噻唑烷二酮，是口服有效的PPAR-γ选择性激动剂。Darglitazone 可以有效控制血糖和脂质代谢，在 II 型糖尿病中有研究价值。

MitoPBN is a mitochondria-targeted antioxidant. It accumulates in the mitochondria following the generation of a mitochondrial membrane potential by succinate, an effect that is blocked by addition of the mitochondrial membrane potential uncoupler FCCP . MitoPBN inhibits superoxide activation of mitochondrial uncoupling protein 1 (UCP1), UCP2, and UCP3 when used at a concentration of 250 nM in vitro but does not react with superoxide. It traps hydroxyl (IC50 = ~77 μM) and carbon-centered radicals and inhibits the initiation of lipid peroxidation in isolated bovine heart mitochondria.

Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial cells and accumulated in the cytosol in a biphasic manner[1]. During pelleting hypoxia, Ru360 (10 µM) significantly improves cell viability in wild type cardiomyocytes[3]. Ru360 (15-50 nmol/kg) treatment abolishes the incidence of arrhythmias and haemodynamic dysfunction elicited by reperfusion in a whole rat model. Ru360 administration partially inhibits calcium uptake, preventing mitochondria from depolarization by the opening of the mitochondrial permeability transition pore (mPTP)[1]. [1]. G de J García-Rivas, et al. Ru360, a Specific Mitochondrial Calcium Uptake Inhibitor, Improves Cardiac Post-Ischaemic Functional Recovery in Rats in Vivo. Br J Pharmacol. 2006 Dec;149(7):829-37. [2]. M A Matlib, et al. Oxygen-bridged Dinuclear Ruthenium Amine Complex Specifically Inhibits Ca2+ Uptake Into Mitochondria in Vitro and in Situ in Single Cardiac Myocytes. J Biol Chem. 1998 Apr 24;273(17):10223-31. [3]. Lukas J Motloch, et al. UCP2 Modulates Cardioprotective Effects of Ru360 in Isolated Cardiomyocytes During Ischemia. Pharmaceuticals (Basel). 2015 Aug 4;8(3):474-82.