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Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and associated signaling pathways. As the orotate salt form of Carboxyamidotriazole (CAI), it is an orally bioavailable signal transduction inhibitor with in vitro antileukaemic activity, exhibiting anti-tumor, anti-inflammatory, and antiangiogenic effects.

Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It shows anti-inflammatory, anti-tumor, and antiangiogenic effects.

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

CAI/II-IN-13 (Compound 5f) is a CAI/II inhibitor with IC50 values of 309.16 nM for hCA I and 267.27 nM for hCA II. It exhibits potent and selective antiproliferative activity against A549 lung cancer cells (IC50 = 0.58 μM). CAI/II-IN-13 is applicable for lung cancer research.

CAI/II-IN-12 is a potent dual inhibitor of hCAI (IC50= 7.12 μM, Ki= 9.26 μM) and hCAII (IC50= 10.62 μM, Ki= 11.72 μM). It exhibits strong affinity for the active sites of CYP17A1, hCAI, and hCAII enzymes. CAI/II-IN-12 demonstrates rapid conformational stabilization, especially in the CYP17A1 complex, and is applicable in prostate cancer treatment and glaucoma research.

CAI-IN-6 (Compound 3F) is an inhibitor of carbonic anhydrase (CAI), exhibiting a Ki of 902.1 nM for hCA I and 86.1 nM for hCA II. It is useful in research related to diuretics, glaucoma, epilepsy, and tumors.

CAI-1 is a vibrio cholerae quorum-sensing autoinducer.

CAI0019 is an orally active α-carbonic anhydrase inhibitor based on the Acetazolamide framework. This compound has narrow-spectrum activity against enterococci, with a MIC50 of 0.094 μM and a MIC90 of 0.39 μM. In a mouse model of septic peritonitis, CAI0019 selectively inhibits enterococci without affecting most gut commensal bacteria.

Droxicainide is an antiarrhythmic agent, [used] to treat irregular heartbeats.

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.

Ketocaine(Rec 7-0518) is a local anesthetic commonly used in animal experiments with potential antitumor activity for pain relief.

Quinacainol (RP 54272) is a new antiarrhythmic compound with class I antiarrhythmic effects in rats.

Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.

Etidocaine is an amino acidamide that acts as a local anesthetic with fast onset and long-acting properties.

Indecainide (Ricainid) is a novel antiarrhythmic compound that is carcinogenic and can be used to study chronic stable ventricular arrhythmias secondary to coronary artery disease or cardiomyopathy.

Vadocaine (Vadocaina) is a novel analgesic compound for local anaesthesia and can be used to study the central nervous system and cardiovascular system.

Recainam is a novel, orally available compound with potent class I antiarrhythmic activity.

solpecainol is a sodium channel blocker used in the study of neurological and cardiovascular diseases.

Trapencaine is a newly synthesized carbamate type local anesthetic that induces conformational changes in sodium channels on hypertrophic cell membranes.

Pincainide is a novel beta-aminoaniline that inhibits, in a dose-dependent manner, diseases caused by abnormal norepinephrine vascular smooth muscle function.

Pilsicainide HCl (SUN 1165) is a pure sodium channel blocker

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.

Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.

Bupivacaine hydrochloride (Vivacaine) is a long-acting, amide-type local anesthetic. Bupivacaine hydrochloride reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.