direct

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

C.I.Direct Blue 199 is a reagent used in biochemical reactions.

Ceruletide is a decapeptide that serves as a safe and effective cholecystokinin receptor agonist, exerting a direct spasmogenic effect on the gallbladder muscle and bile ducts, and is commonly used to establish pancreatitis models.

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.

Melagatran is an orally available, direct synthetic thrombin inhibitor that does not require endogenous cofactors other than thrombin and does not significantly interact with any other enzymes in the coagulation cascade or with the fibrinolytic enzymes.

3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells.

Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell.

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1) programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1 PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1 PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

Itaconate-alkyne (ITalk) is a bioorthogonal probe for quantitative, site-specific chemoproteomic profiling of itaconate in inflammatory macrophages, facilitating biochemical evaluation and proteomic analysis of its direct targets.

MC-1-F2 is a direct FOXC2 inhibitor with anticancer activity, inhibits cancer stem cell (CSC) characteristics, and reduces the invasive ability of castration-resistant prostate cancer (CRPC) cell lines. MC-1-F2 can be used to study prostate cancer.

BMS-593214 is an active site-directed factor (F) VIIa inhibitor that exhibits antithrombotic and antihaemostatic properties. It acts as a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of FVIIa-activated substrate FX. Additionally, BMS-593214 effectively prevents electroinduced carotid artery thrombosis (AT) and wire-induced vena cava thrombosis (VT).

Isoxsuprine hydrochloride (Isolait) is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle.

Cyclandelate (BS 572), a direct-acting smooth muscle relaxant, is used to dilate blood vessels.

Norepinephrine bitartrate monohydrate is an effective adrenergic receptor (AR) agonist that directly activates α1, α2, and β1 receptors, and is commonly used to induce cardiomyopathy models.

3-Pyridinemethanol (Roniacol) is an alcohol analog of NICOTINIC ACID which is a direct-acting peripheral vasodilator that causes flushing and may decrease blood pressure. It is used in vasospasm and threatened GANGRENE.

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.

L-Glutamic acid is an excitatory amino acid neurotransmitter and a Glutamic acid receptor agonist, including metabolic glutamic acid receptor (mGluR), AMPA receptor, NMDA receptor and KA receptor. L-Glutamic acid has an excitatory effect on the process of DA release from dopaminergic nerve endings. L-Glutamic acid can be used in the research of neurological diseases. L-Glutamic acid acts on ionic and metabolic Glutamic acid receptors.

5-Hydroxytryptophan (NSC-92523) is a metabolite of tryptophan and a direct precursor of serotonin. It is a substrate of aromatic amino acid decarboxylase and can be used to induce depression models.

Velpatasvir (GS-5816), also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Dantrolene sodium hemiheptahydrate (Sodium dantrolene) is the sodium salt form of dantrolene, a hydantoin derivative, and direct-acting skeletal muscle relaxant.

N-Nitroso-N-methylurea (NMU/MNU/NMH) is a nitrosourea compound with alkylating, carcinogenic, and mutagenic properties; as a direct-acting alkylating agent, it interacts with DNA and targets multiple animal organs to induce various cancers and degenerative diseases, and is commonly used to induce disease models such as gastric cancer and breast cancer in mice.

Pyrrole-2-carboxylic acid (Minaline) was first identified as a degradation product of sialic acids, then as a derivative of the oxidation of the D-hydroxyproline isomers by mammalian D-amino acid oxidase. The latter relationship results from the lability of the direct oxidation product, A'-pyrroline-4-hydroxy-2-carboxylic acid, which loses water spontaneously to form the pyrrole. A similar reaction is catalyzed by the more specific allohydroxy-D-proline oxidase of Pseudomonas. In whole animal observations, pyrrole-2-carboxylate (PCA) ' was identified in rat or human urine after administration of the D-isomers of hydroxyproline, a finding ascribable to the action of D-amino acid oxidase. Urinary excretion of N-(pyrrole-2-carboxyl) glycine has been reported in a 5-year-old affected with type II hyperprolinemia; The child has mild developmental delay, recurrent seizures of the grand mal type and EEG alterations.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).