Calcium Channel Inhibitor

Multi-kinase-IN-10 (Compound IIIk) is a multi-kinase inhibitor. Multi-kinase-IN-10 exhibits significant calcium channel blocking activity, with its IC₅₀ being 26.67 μM. Multi-kinase-IN-10 is a potent dual cholinesterase inhibitor, with its IC₅₀ values for hAChE and hBuChE being 0.304 μM and 1.033 μM respectively. Multi-kinase-IN-10 has antioxidant and neuroprotective activities, and shows significant anti-amnesia activity. Multi-kinase-IN-10 can be used for research on Alzheimer's disease.

ω-Tbo-IT1 is a peptide toxin that can be isolated from the venom of Tibellus oblongus.ω-Tbo-IT1 is an inhibitor of insect calcium channel.

ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca²⁺ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.

UK 52831 is a long acting dihydropyridine calcium channel antagonist. UK 52831 can be used for cardiovascular disease (such as hypertension and myocardial ischemia) and anti-inflammatory research.

Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrobromide is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine hydrobromide significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine hydrobromide not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine hydrobromide exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine hydrobromide may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine hydrobromide can be used in research related to hypertension and atherosclerosis.

LY393615 (NCC1048) is a novel neuronal Ca²⁺ (calcium channel) and Na ⁺ channel (sodium channel) blocker with IC₅₀s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research.

L-Ascorbic acid calcium dihydrate (L-Ascorbate calcium dihydrate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid calcium dihydrate inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid calcium dihydrate is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid calcium dihydrate exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

Leualacin, a calcium channel blocker, can be isolated from the fungus Hapsidospora irregularis.

Nisoldipine-d₃ is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.

Dronedarone-d₆ (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.

ONO-2921 is an orally active and selective N-type calcium channel blocker. ONO-2921 functionally blocks N-type calcium channels. ONO-2921 reduces paw withdrawal responses during persistent nociception and hyperalgesia to heat in neuropathic pain models. ONO-2921 can be used for research on neuropathic pain and nociceptive pain.

T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC₅₀s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC₅₀s of 5.0, 6.4 µM, respectively.

Cilnidipine-d₇ is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.

GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC₅₀ of 3 μM by using Ba²⁺ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells.

LQFM020 is an orally active pyrazole derivative. LQFM020 inhibits Ca⁺ and activates K⁺ and NO/cGMP channels to inhibit vasoconstriction. LQFM020 has anti-inflammatory and anti-analgesic activities.

GTx1-15 is an inhibitor cystine knot (ICK) peptide that inhibits the voltage-dependent calcium channel Cav3.1 and the voltage-dependent sodium channels Nav1.3 and Nav1.7.

Norfluoxetine hydrochloride (Standard) is the analytical standard of Norfluoxetine hydrochloride (HY-W011235). This product is intended for research and analytical applications. Norfluoxetine hydrochloride is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine hydrochloride exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine hydrochloride inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine hydrochloride can be used in research related to depression, ischemic stroke, and epilepsy.

Methyl isoplatydesmine is a cholinesterase inhibitor with spasmolytic activity, with a K_i value of 30.0 μM against electric eel acetylcholinesterase and a K_i value of 19.0 μM against horse serum butyrylcholinesterase. Methyl isoplatydesmine mediates spasmolytic activity by blocking voltage-dependent calcium channels. Methyl isoplatydesmine can be used in the research of Alzheimer's disease and related dementias.

Ranolazine-d₈ (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.

Norverapamil (hydrochloride) (Standard) is the analytical standard of Norverapamil (hydrochloride). This product is intended for research and analytical applications. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].