act-2

ACT-209905 is an agonist of S1P1 receptor.

ACT-280778 is a potent L T calcium channel blocker.

ACT-281959, a prodrug of ACT-246475, is a novel potent and selective P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel. ACT-281959 showed antithrombotic efficacy after oral administration in the rat ferric chloride model. ACT-281959 entered clinical studies in healthy volunteers.

RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

5-Methyl-2'-deoxycytidine (5MedCyd) is a pyrimidine nucleoside that when incorporated into single-stranded DNA can act in cis to signal de novo.

MFCD01917484 (ETHYL 2-AMINO-4-(4-METHOXYPHENYL)-3-THIOPHENECARBOXYLATE) is a derivative of thiophene that possesses a variety of properties, including the ability to act as a ligand, catalyst and photosensitizer. It has been used as a model compound for biochemical and physiological studies as well as drug discovery and development.

AZD4547 is an FGFR family inhibitor. AZD4547 selectively inhibits FGFR1 phosphorylation and suppresses cancer cell proliferation through inhibition of FGFR1 signaling, and is able to act on FGFR1 (IC50:0.2 nM), FGFR2 (IC50:2.5 nM), FGFR3 (IC50:1.8 nM) and FGFR4 (IC50:165 nM). IC50:165 nM).[2]

Morroniside would act as a regulator of hepatic inflammatory reactions and lipid metabolism in db db mice. It exhibits protective effects against diabetic renal damage and human umbilical vein endothelial cells, by inhibiting hyperglycemia and oxidative s

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

2-Hydroxymethyl-5-hydroxypyridine is a natural product isolated from the mature and dried seeds of S. lychnophora.2-Hydroxymethyl-5-hydroxypyridine can act as a kinase inhibitor.

ACT-389949 is a potent and selective agonist of formyl peptide receptor type 2 (FPR2) Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2 ALX internalization into monocytes. It has the potential for the treatment of inflammatory disorders.

Ascr#2 (asc-C6-MK) is a glycoside analogue in Cryptococcus hidradii that promotes dauer formation.Ascr#2 mixtures with ascr#3 at low concentrations act as a male elicitor and can be used to detect population density.Ascr#5 (asc-ωC3) is a highly conserved ascaroside analogue in Cryptococcus hidradii that regulates a variety of responses in Cryptococcus hidradii.

Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1) orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

ACT-462206 is an orally available Orexin 1 Orexin 2 receptor antagonist that crosses the blood-brain barrier.ACT-462206 is highly potent and can be used in studies of sleep and anxiety.

Momordin Ic (Momordin 1c) might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MAPK and PI3K-mediated iNOS and HO-1 pathways. Also, Momordin Ic accelerates gastrointestinal transit partially by stimulating synthesis of 5-HT to act through 5-HT(2), which, in turn, increases synthesis of prostaglandins.

Ganglioside GD1a is a sialic acid-containing glycosphingolipid found in brain, erythrocytes, bone marrow, testis, spleen, and liver. [1] It can be shed from the surface of tumor cells into the microenvironment where it influences tumor-host cell interactions to promote tumor cell proliferation, invasion, and metastasis. Ganglioside GD1a (20 μM) also increases endothelial cell proliferation. Furthermore, ganglioside GD1a has been shown to act as a functional coreceptor for toll-like receptor 2 (TLR2), enabling the recruitment of TLR2 to lipid rafts when bound by a bacterial toxin.[2] Ganglioside GD1a mixture contains ganglioside GD1a molecular species with C18:1 and C20:1 sphingoid backbones.

Coenzyme Q10 is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP. In its reduced form, it acts as an antioxidant. Coenzyme Q2 is a precursor of coenzyme Q10 that has 2, rather than 10, isoprenoid units on the ubiquinone base. It can act as an electron acceptor for bacterial Complex I. In mammalian cells, exogenous coenzyme Q2 prevents the production of reactive oxygen species associated with Complex I activity. Forms of coenzyme Q with shorter isoprenoid chains, including coenzyme Q2, induce p53-dependent apoptosis in human B-cell acute lymphoblastoid leukemia BALL-1 cells.

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity.[1] At a 25 uM concentration, PGA2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase .[2] It has also been shown to act as a vasodilator with natriuretic properties.[3]

The inositol phosphates (IPs) are a family of molecules produced by altering the phosphorylation status of each of the six carbons on the cyclic inositol structure. They act as second messengers, regulating a wide array of cellular functions. D-myo-inositol-1,3,4,6-tetraphosphate(Ins(1,3,4,6)-P4) largely acts an intermediate, serving as substrate for inositol-1,3,4,6-tetraphosphate 5-kinase to produce inositol-1,3,4,5,6-pentaphosphate, or inositol-1,3,4,6-tetraphosphate 2-kinase to give inositol-1,2,3,4,6-pentaphosphate. These inositol pentaphosphates can be further phosphorylated to produce inositol-1,2,3,4,5,6-hexakisphosphate, or phytic acid, which serves diverse roles in eukaryotic tissues. Ins(1,3,4,6)-P4 is a poor activator of the inositol 1,4,5-trisphospate receptor in vitro. Other functions of this IP remain to be elucidated.

17-oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-Docosahexaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DHA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).