syndrome

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.

GSK1940029 (SCD inhibitor 1) is an inhibitor of stearoyl-CoA desaturase (SCD).

Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Pramipexole (SND 919) is a selective dopamine receptor agonist used in the therapy of Parkinson disease. Pramipexole therapy is associated with a low rate of transient serum enzyme elevations during treatment but has not been implicated in cases of clinically apparent acute liver injury.

Pramipexole dihydrochloride hydrate (Mirapex) is the hydrochloride salt of pramipexole, a benzothiazole derivative. As a nonergot dopamine agonist, pramipexole binds to D2 and D3 dopamine receptors in the striatum and substantia nigra of the brain.

Zamifenacin fumarate (UK-76654 fumarate) is a potent, gut-selective antagonist of the muscarinic M3 receptor.

11-Beta-hydroxyandrostenedione (NSC-17102) is a steroid mainly found in the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue), which is a 11β-hydroxysteroid dehydrogenase isozymes inhibitor. Measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism with 4-androstenedione increases.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

Dicyclomine hydrochloride is a muscarinic antagonist used as an antispasmodic and in urinary incontinence.

Tegaserod maleate (SDZ-HTF-919) is a 5-HT4 agonist manufactured by Novartis for managing irritable bowel syndrome and constipation. It was the only drug approved by the United States Food and Drug Administration for relieving abdominal discomfort, bloating, and constipation associated with irritable bowel syndrome. On March 30, 2007, the FDA requested that Novartis withdraw Zelnorm from the market due to alleged increased risks of heart attack or stroke associated with its use.

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

AZD7325 (AZD-7325) is a GABA-Aα2,3 -selective receptor modulator.

Blarcamesine (AVex-73) is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease.

HRO761 is a potent Werne r syndrome RecQ DNA deconjugase (WRN) inhibitor that can be used to study cancers such as colon and stomach cancer.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Fenclonine (CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine(CP-10188) acts pharmacologically to deplete endogenous levels of serotonin.

Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.