action

12-oxo-N-[1-(propan-2-yl)piperidin-4-yl]-6H,7H,8H,9H,10H,12H-azepino[2,1-b]quinazoline-3-carboxamide available as a molecular structural unit, it is used in the synthesis of various compounds.

B7/CD28 interaction inhibitor 1 (CTLA-4 inhibitor) is a potent CTLA-4 inhibitor.

Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.

Acecainide hydrochloride (NAPA) is a major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.

Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) . BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker. The mechanism of action of irbesartan is as an Angiotensin 2 Receptor Antagonist.

Cilostazol (OPC 21) is a Phosphodiesterase 3 Inhibitor. The mechanism of action of cilostazol is as a Phosphodiesterase 3 Inhibitor.

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

5'-Guanylic acid disodium salt (GMP-5) belongs to the class of organic compounds known as purine ribonucleoside monophosphates. In particular, L-Glutamic acid and guanosine monophosphate can be biosynthesized from xanthylic acid and L-glutamine; which is catalyzed by the enzyme GMP synthase [glutamine-hydrolyzing]. In addition, Guanosine triphosphate and guanosine monophosphate can be biosynthesized from diguanosine tetraphosphate; which is catalyzed by the enzyme bis(5'-nucleosyl)-tetraphosphatase [asymmetrical]. In humans, guanosine monophosphate is involved in the kanamycin action pathway, the telithromycin action pathway, the tobramycin action pathway, and the erythromycin action pathway. Guanosine monophosphate is also involved in several metabolic disorders, some of which include the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria (D and L form) pathway. Outside of the human body, guanosine monophosphate can be found in a number of food items such as onion-family vegetables, millet, chinese water chestnut, and red rice. This makes guanosine monophosphate a potential biomarker for the consumption of these food products.

Sulfamethoxazole (STX 608) is a Sulfonamide Antimicrobial. The mechanism of action of sulfamethoxazole is as a Cytochrome P450 2C9 Inhibitor. The chemical classification of sulfamethoxazole is Sulfonamides.

Letrozole (CGS 20267) is an Aromatase Inhibitor. The mechanism of action of letrozole is as an Aromatase Inhibitor.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Triamcinolone acetonide (Azmacort) is a Corticosteroid. The mechanism of action of triamcinolone acetonide is as a Corticosteroid Hormone Receptor Agonist. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Bergenin (Bengenin) is a polyphenol, which is an effective antinarcotic agent with antioxidant action.

Azelaic acid (Anchoic acid) is a component of hair and skin conditioners and is produced by the ozonolysis of oleic acid. Azelaic acid has bacteriostatic activity against Propionibacterium acnes and Staphylococcus epidermidis by inhibiting protoprotein synthesis in microbial cells. Azelaic acid also has the ability to inhibit pigmentation due to its free radical scavenging action.

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

Methyl nicotinate (methyl pyridine-3-carboxylate) is the methyl ester of that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.

Glycoursodeoxycholic acid (Ursodeoxycholylglycine) is an acyl glycine and a bile acid-glycine conjugate. It is a secondary bile acid produced by the action of enzymes existing in the microbial flora of the colonic environment. In hepatocytes, both primary and secondary bile acids undergo amino acid conjugation at the C-24 carboxylic acid on the side chain, and almost all bile acids in the bile duct, therefore, exist in a glycine conjugated form. Bile acids are steroid acids found predominantly in bile of mammals.

Indomethacin (Indometacin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.

1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic.

Orlistat (Tetrahydrolipstatin) is an Intestinal Lipase Inhibitor. The mechanism of action of orlistat is as a Lipase Inhibitor.

Ostarine (MK-2866) is a non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. 2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors. 3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Ambroxol hydrochloride (Mucosolvan) is a metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride.

Beclin1-ATG14L Interaction Inhibitor 1 (COM 19) is a selective inhibitor targeting the specific interaction between Beclin1 and ATG14L. It impedes the formation of complex I in the lipid kinase VPS34, thus inhibiting autophagy, while leaving complex II intact, which relies on the Beclin 1-UVRAG interaction for its integrity and is essential for vesicle transport [1].

Antitumor Agent-108 (Compound 5), an inhibitor of the Hyaluronic Acid (HA)-CD44 interaction, effectively disrupts cancer spheroid integrity and exhibits antiproliferative activity against cancer cells [1].

SORT-PGRN Interaction Inhibitor 2 is a compound that downregulates SORT1 protein expression and enhances extracellular progranulin (PGRN) secretion in various mammalian cell lines, and is utilized in the study of neurological diseases [1].

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].

Antitumor agent-109 (compound 6) is a dual-function inhibitor that targets hyaluronic acid and CD44, which are involved in tumor progression and invasion. It demonstrates potent antitumor activity, specifically inhibiting MDA-MB-231 cells with an EC50 of 0.59 µM [1].

Hydrazinium hydroxide is a fluorinated carboxylic acid that has been used to study the mechanisms of action of enzymes, hormones and other biomolecules. It has also been used to study the effects of various drugs on the body and to study the effects of environmental toxins on the body.

Hemopressin (rat) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB2 cannabinoid receptors. Hemopressin exerts antinocicep

Prifinium bromide is a quaternary ammon antimuscarinic. It inhibits hyperkinesia of the digestive organs and urinary tract and has a spasmolytic action.

Anagrelide (Xagrid) is a Platelet-reducing Agent. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by means of Decreased Platelet Production.

Izonsteride (LY320236) is a selective and potent 5alpha reductase inhibitor with dual action on the type I and type II isoforms of the enzyme.Izonsteride is used in the treatment of oncology and genitourinary disorders, and may be used in the study of prostate cancer.

Vasopressin acetate, a cyclic nonapeptide, is synthesized centrally in the hypothalamus. Vasopressin acetate acts as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.

L-Sophoridine (Matridin-15-one) , a natural product obtained from medicinal plants, which has a variety of pharmacological effects, including anti-Y effects, and selectively induces apoptotic cell death in a variety of human Y cells in vitro and in vivo; however, its mechanism of action needs to be further elaborated.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

CBiPES hydrochloride (CBiPES HCl) is a potent orthosteric modulator of the mGlu2 receptor with an EC50 value of 92.8 nM.CBiPES hydrochloride blocks the action of WT and mGlu(3) receptors.CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome. CBiPES hydrochloride can be used to study neurological disorders like epilepsy and Parkinson's syndrome.

Peptide T acetate is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a synthetic octapeptide whose possible mechanism of action is the competitive inhibition of gp120 to the CD4 receptor as well as binding to vasointestinal peptide receptors and inhibiting cytokine action

Tiaramide hydrochloride (FK-1160) is an anti-inflammatory drug that inhibits the action of mediators released from mast cells and has direct smooth muscle relaxant properties.

SBI993 is an analog of SBI-477 and can be used as a biomarker to confirm the expected action of MondoA target gene expression in vivo. SBI993 reduces muscle TAG levels and hepatic steatosis.