states

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

Gluconate Calcium (Gluconic acid hemicalcium salt) is the calcium salt of gluconic acid, used as a calcium replenisher in hypocalcemic states.

Florfenicol (Aquafen) is a fluorinated synthetic analog of thiamphenicol. In the United States, florfenicol is currently used to treat bovine respiratory disease (BRD) associated with Mannheimia (Pasteurella) haemolytica, Pasteurella multocida, and Haemophilus somnus, to treat bovine interdigital phlegmon associated with Fusobacterium necrophorum and Bacteroides melaninogenicus.

Florfenicol (SCH-25298), a fluorinated synthetic analog of thiamphenicol, is currently indicated for the therapy of bovine respiratory disease (BRD) associated with Mannheimia (Pasteurella) haemolytica, Haemophilus somnus, and Pasteurella multocida, for therapy of bovine interdigital phlegmon (foot rot, infectious pododermatitis, acute interdigital necrobacillosis) associated with Fusobacterium necrophorum and Bacteroides melaninogenicus. This compound is also used in aquaculture and is approved for use in the United States for the therapy of enteric septicemia in catfish.

Amisulpride (DAN 2163) (trade name Solian) is an antipsychotic drug sold by Sanofi-Aventis. It is not approved for use in the United States, but is approved for use in Europe and Australia for the treatment of psychoses and schizophrenia. Additionally, it is approved in Italy for the treatment of dysthymia (under the brand name Deniban). Amisulpride is a selective dopamine antagonist.

Terpin hydrate, a cis-form hydrate, is derived from sources such as oil of turpentine, oregano, thyme, and eucalyptus. It is used as an insect repellent and expectorant. Terpin hydrate(cis-Terpin hydrate) is commonly used to loosen mucus and ease congestion in patients presenting with acute or chronic bronchitis, and related pulmonary conditions. It was popular in the United States since the late nineteenth century, but was removed from marketed medications in the 1990s after the U.S. Food and Drug Administration (FDA) stated that based on the evidence currently available, there are inadequate data to establish general recognition of the safety and effectiveness of these ingredients . Elixirs of terpin hydrate are still available with a prescription but must be prepared by a compounding pharmacy.

Bromopride (Valopride) is a dopamine antagonist with prokinetic properties closely related to metoclopramide, and is widely used as an antiemetic. It is not available in the United States or the United Kingdom.

Pizotifen (Pizotyline) is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. It also possesses sedative and appetite-stimulating properties. Pizotifen hydrochloride is an active ingredient in Sandomigran, which is used for the prophylactic management of migraine. Sandomigran is available in number of countries excluding the United States.

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

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.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

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.

Bedaquiline (R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis.

Potassium Channel Activator 1 can be used in studies about the treatment of disorders or conditions wherein the dopaminergic system is disrupted such as mood disorders ADHD, schizophrenia, and other psychotic states.

Ormetoprim (Ro 5-9754), an antibiotic approved for use in the United States, is used to prevent the spread of disease in freshwater aquaculture.

Isoxicam (Isoxicamum) is a non-steroidal anti-inflammatory drug that is not marketed in the United States.

Minaprine, a reversible inhibitor of MAO-A, is used in the treatment of various depressive states.

LY88074 Methyl ether is effective in inhibiting conditions associated with estrogen deprivation syndrome, such as osteoporosis and hyperlipidemia, which occur due to various estrogen-deficient states.

COX 5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.

Pericyazine (Propericiazine) is a selective D2-dopamine receptor antagonist. Pericyazine is a first-generation antipsychotic drug that is used as an adjunct to the short-term management of severe anxiety states and psychosis.

D-2-Phosphoglyceric acid is a crucial metabolic intermediate known for its role in enhancing cellular energy metabolism and regulating biosynthesis. It plays a key role in both glycolysis and photosynthesis, which are essential for cellular energy supply. Additionally, D-2-Phosphoglyceric acid serves as a biomarker for monitoring metabolic states in various organisms.

JNJ-41443532 Free Base is an oral CCR2 receptor antagonist used in the treatment of type 2 diabetes. The compound has completed a Phase I trial with healthy volunteers in Belgium and a Phase II trial involving type 2 diabetes patients in the United States.