blocker

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.

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.

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.

(+)-KCC2 blocker 1 is a selective inhibitor of KCC2 with an IC50 of 0.4 μM.

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).

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.

Cav 2.2 3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC50 values of 1.22 μM for Cav2.2 and 80 μM for Cav3.2, capable of penetrating the central nervous system.

NMO-IgG blocker A-01 is a idiotype-specific blocker of neuromyelitis opticaimmunoglobulin g (nmo-igg) binding to aquaporin-4 (aqp4)

NaV1.2 1.6 channel blocker-1 is a potent inhibitor of NaV1.2 and NaV1.6 channels, exhibiting inhibitory effects on rNaV1.6 and hNaV1.2. This compound can be utilized in the study of generalized epilepsy and movement disorders.

TRPV2-selective blocker 1 (compound IV2-1) is a selective inhibitor of the TRPV2 channel, with an IC50 value of 6.3 μM, specifically targeting the TRPV2 channel without affecting TRPV1, TRPV3, or TRPV4 channels, and effectively suppresses TRPV2-mediated calcium influx in macrophages, inhibiting their phagocytic activity [1].

MTDH-SND1 Blocker 1 (Compound C26-A6) serves as an inhibitor targeting the MTDH-SND1 protein, effectively suppressing cancer metastasis [1].

Nav1.7 blocker 1 (example 41), an effective Na+ channel (Na v) blocker, exhibits a potent IC50 value of 0.037 μM. This compound is utilized in pain research, encompassing neuropathic, postoperative, and inflammatory pain among others [1].

Abeprazan hydrochloride (Fexuprazan hydrochloride) is an effective reversible potassium-competitive acid blocker with oral activity, inhibiting H+, K+ -atPase by competitive binding to potassium ions without acid activation. Abeprazan hydrochloride is a proton pump inhibitor (PPI) that acts by reducing gastric acid production and is used to treat gastric acid-related disorders, such as gastroesophageal reflux disease (GERD) and peptic ulcers.

Bucindolol Formatel is a blocker of β1-adrenergic receptor. Bucindolol exhibits intrinsic sympathomimetic activity. Bucindolol can be used in the research of heart failure.

JTV-519 Formate is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA). JTV-519 Formate is also a partial agonist of ryanodine receptors in striated muscle. JTV-519 Formate exhibits antiarrhythmic and cardioprotective properties.

McN5691 (RWJ26240) is a voltage-dependent calcium channel blocker with antihypertensive activity that can be used in the study of diseases caused by vascular smooth muscle abnormalities.

PD0176078 () is a newly blocker of N-type Calcium channel.