BL-1249 is a putative activator of potassium TREK-1 channel. BL-1249 produced a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 uM) or by direct electrophysiological measurement (EC50 = 1.49 +/- 0.08 uM). BL-1249 also produced a membrane hyperpolarization of acutely dissociated rat bladder myocytes. Voltage-clamp studies in human bladder cells revealed that BL-1249 activated an instantaneous, noninactivating current that reversed near E(K). BL-1249 behaves as a potassium channel activator that exhibits bladder versus vascular selectivity both in vitro and in vivo.

Isosorbide 2-mononitrate is a pharmacologically active metabolite of isosorbide dinitrate, an organic nitrate isosorbide dinitrate indicated for the prevention of angina pectoris due to coronary artery disease. It activates guanylate cyclase.

α-D-Fucopyranose (aka α-D-fucose) is a six-carbon deoxy monosaccharide. It is equivalent to 6-deoxy-D-galactose. It acts as a non-metabolizable analog of L-arabinose and inhibits induction of the L-arabinose operon in some bacteria. Other bacteria possess a mutant araC gene where D-fucose acts as a gratuitous inducer of the L-arabinose operon. D-fucose also acts as an activator of the galS promotor in E. coli. Because of its ability to regulate gene expression, there has been some interest in exploring D-fucose as a lead compound in neurodegenerative diseases or cancer.

Sinomenine is a pure alkaloid extracted from the Chinese medical plant Sinomenium acutum. Caulis Sinomenii is the dried plant stems of Sinomenium acutum and Sinomenium acutum var. cinereum and has been used in Chinese medicine for treating rheumatic diseases for over a thousand years. Sinomenine possesses the anti-arthritic effect, that may be related to the suppression of both Th1 (T-helper 1) and Th2 immune responses, also this potential drug can be used to treat allergic rhinitis, and the mechanism may rely on the improvements of the Th1/Th2 imbalance. In addition, Sinomenine displays antinociceptive activity, possibly through activation of the μ-opioid receptor. Also was discovered, sinomenine significantly improves cardiac function in diabetic rats, which may be attributed to the deactivation of NF-κB and the blockade of inflammatory cytokine-mediated immune reactions.

NS3623 is a human ether-a-go-go (hERG) KV11.1 potassium channel activator. It was shown that treatment of transgenic mouse model of sickle cell disease (SAD mice) with NS3623 improves erythrocyte hydration and diminishes sickling, probably by lowering of the Cl-conductance, which limits salt and concomitant water loss mediated by the Gardós channel, that makes NS3623 antisickling agent in vivo

Cucurbitacin E (CuE), a potent member of triterpenoid family isolated from plants, has been confirmed as an antitumor agent by inhibiting proliferation, migration, and metastasis in diverse cancer. Cucurbitacin E nhibits OS tumor growth and invasion through inhibiting the PI3K/Akt/mTOR signaling pathway. CuE can be considered to be a promising anticancer agent for OS. Cucurbitacin E exerts anti-inflammatory actions. It inhibited both COX enzymes with more selectivity toward COX-2. CuE has been reported to possess anti-inflammatory and anti-tumorigenic properties mediated by its action on the cellular cytoskeleton, on mitotic pathways as well as on cellular autophagy.

15-Ketoprostaglandin E2 (15-keto PGE2) is a metabolite of prostaglandin E2 (PGE2) with reduced biological activity, which then by the action of prostaglandin reductase 2 (PTGR2) transforms into 13,14-dihydro-15-keto-PGE2, s a secondary metabolite without biological activity. Some experiments have shown that exists the therapeutic potential by targeting PTGR2/15-keto-PGE2 in pancreatic cancer. Besides, it is known, that 15-keto-PGE2 has higher affinity to the prostaglandin EP2 receptor than to the EP4 receptor. Some experiments also have revealed the key signaling cascade: 15-Hydroxyprostaglandin dehydrogenase (15-PGDH)/15-keto-PGE2-mediated activation of PPARγ and p21(WAF1/Cip1) in the regulation of the hepatocarcinogenesis and tumor progression.