blocker

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

Oxcarbazepine (GP 47680) is an Anti-epileptic Agent. The physiologic effect of oxcarbazepine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

Nicardipine hydrochloride (YC-93 Hydrochloride) is the hydrochloride salt form of nicardipine, a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.

Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.

Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats. Fenamic acid serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including flufenamic acid, tolfenamic acid, mefenamic acid, and meclofenamic acid.

Clodronate disodium tetrahydrate (Clastoban) inhibits bone resorption and soft tissue calcification.

Nicardipine (Cardene), a calcium channel blockers belonging to the dihydropyridine class, is a drug used to treat angina and high blood pressure.

Sematilide hydrochloride (CK-1752) is a class III antiarrhythmic. It is a selectively delayed rectifier K+ current (IKr) channel blocker. It inhibits rapidly activating Ik in guinea pig atrial myocytes, resulting in the prolongation of refractoriness and action potential duration.

1. Oxypeucedanin ((+-)-Oxypeucedanin) has novel anticancer effect, mediated via induction of G2-M cell cycle arrest and apoptosis in human prostate carcinoma DU145 cells. 2. Oxypeucedanin is a kind of open-channel blocker of the hKv1.5 channel and it prolongs the APD; therefore, it is an excellent candidate as an antiarrhythmic drug for atrial fibrillation.

Sevelamer carbonate is a non-absorbed phosphate binding crosslinked polymer, with the same polymeric structure as sevelamer hydrochloride, in which carbonate replaces chloride as the counterion.

Vonoprazan (TAK-438 (free base)) is an orally active potassium-competitive acid blocker.Vonoprazan can be used for the treatment of gastroduodenal ulcer and reflux esophagitis

Butacaine is a local anesthetic.

DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with IC50 of 0.64 μM, which is expected to block the absorption of iron by intestinal cells in vivo.

Cav 2.2 blocker 1 is an N-type calcium channel (Cav 2.2; IC50: 1 nM) blocker for the treatment of pain.

DMT1 blocker 2, compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 hydrogen peroxide value of 0.83, which is expected to block iron uptake by intestinal epithelial cells in vivo.

M2 ion channel blocker ,Antiviral agent, is capable of inhibiting and blocking the activity of M2 ion channel.

N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.

MTDH-SND1 blocker 2 (compound C19) is an effective MTDH-SND1 inhibitor with an IC50 value of 487 nM. It binds to the SND1 protein with a Kd of 279 nM and can degrade the SND1 protein. Additionally, MTDH-SND1 blocker 2 exhibits antiproliferative activity and induces apoptosis, showing potential for breast cancer research.

Cav 3.1 blocker 1 (compound 12) is a T-type calcium channel inhibitor with an IC50 value of 160 nM for Cav3.1. It exhibits weaker inhibition on Cav 3.2 with an IC50 of 5000 nM and shows no inhibitory effect on Cav 3.3 and Cav 1.2 (IC50 > 10000 nM).

FAAH/TRPV1 blocker-1 (compound 2R) is a dual blocker of FAAH and TRPV1, exhibiting IC50 values of 0.12 μM and 94.9 μM, respectively. This compound plays a significant role in research focused on pain relief and anti-inflammatory effects.

M2 ion channel blocker-2 (Compound 10) is an inhibitor of the M2 ion channel. It effectively blocks both the wild type and mutant M2 (L27F and V27A) ion channels. This compound exhibits potent antiviral activity against HCoV-229E, with an EC50 of 4.7 μM for cytopathic effect, but shows no efficacy against influenza A virus. Additionally, M2 ion channel blocker-2 does not significantly inhibit hERG or cytochrome P450 enzymes (CYP1A2, CYP2C19, and CYP3A4).

NaV1.7 Blocker-801 is a potent NaV1.7 blocker.

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.