Calcium Channel Inhibitor

3,5,7,3’,4’-Pentamethoxyflavone is a Ca²⁺ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases.

Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC₅₀ of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC₅₀ of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10).

Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC₅₀ of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.

MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC₅₀ of 1.7 μM. MRS1845 is an ORAI1 inhibitor. MRS1845 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis.

Demethylsuberosin (7-Demethylsuberosin) is a coumarin compound found in Angelica gigas Nakai. Demethylsuberosin exerts antihypertensive effects by inhibiting the L-type Ca_V1.2 channel. Demethylsuberosin has antioxidant and anti-inflammatory activities. Demethylsuberosin also exhibits neuroprotective activities against glutamate-induced toxicity in primary cultured rat cortical cells.

Carbamazepine (Standard) is the analytical standard of Carbamazepine. This product is intended for research and analytical applications. Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC₅₀ of 131 μM. Carbamazepine blocks voltage gated Na⁺, Ca²⁺, and K⁺ channels, and is also a HDAC inhibitor (IC₅₀: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.

Linoleamide is a linoleic acid amide. Linoleamide regulates Ca (II) ux and inhibits the erg current.

Levamlodipine ((S)-Amlodipine; Levoamlodipin) besylate is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate 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 besylate 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 besylate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate 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 besylate can be used in research related to hypertension and atherosclerosis.

Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca²⁺ signaling, with an IC₅₀ of 65 nM. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice.

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.

Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W^+/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways.

DPO-1 is a potent Kv1.5 and Kv1.3 (EC₅₀ = 3.1 μM) channels inhibitor with potential immunomodulatory and anti-inflammatory effects. DPO-1 reduces Kv1.3 current density, blunts Ca²⁺ influx in Ca²⁺-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. DPO-1 inhibits Uric acid sodium (HY-B2130A) (MSU)-induced NLRP3 inflammasome activation by blocking Kv1.5-mediated K⁺ efflux. DPO-1 can be used for the study of immunologic disorders and atrial fibrillation.

Catharanthine ((+)-3,4-Didehydrocoronaridine), a constituent of anticancer vinca alkaloids, inhibits voltage-operated L-type Ca²⁺ channel (VOCC). Catharanthine has IC₅₀s of 220 μM and 8 μM for VOCC currents in cardiomyocytes and vascular smooth muscle cells (VSMCs), respectively. Catharanthine lowers blood pressure (BP), heart rate (HR). Catharanthine has anti-cancer activity.

Caloxin 1C2 is a specific PMCA (plasma-membrane Ca²⁺-ATPases) inhibitor. Caloxin 1C2 is selective for PMCA4 over PMCA1, 2 and 3. The K_i values of Caloxin 1C2 are 2.3 μM for PMCA4 and 21 μM for PMCA1. Caloxin 1C2 dose not cause any significant effects on total Ca²⁺ transfer. Caloxin 1C2 affects coronary contractility.

S100P-IN-1 is a S100P inhibitor, and S100P is a calcium-binding protein. S100P-IN-1 potently inhibits the interaction between purified human S100P and RAGE-Fc protein, with an IC₅₀ value of 22.7 nM. S100P-IN-1 exerts anti-metastatic effects on pancreatic cancer cells. S100P-IN-1 can be used for the research of pancreatic cancer.

Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.

Suloctidil is an orally active calcium channel blocker and antifungal agent. Suloctidil antagonizes vasoconstriction induced by norepinephrine, angiotensin and serotonin. Suloctidil inhibits platelet function and exhibits neuroprotective effects. Suloctidil exerts inhibitory effects on Candida albicans biofilm and virulence. Suloctidil can be used in research on vasospasm relief, antithrombosis and superficial candidiasis.

IP3RPEP6 is an IP₃R competitive inhibitor. IP3RPEP6 has the IC₅₀ values of 9.0 μM, 3.9 μM and 4.3 μM for IP₃R1, IP₃R2 and IP₃R3, respectively. IP3RPEP6 does not affect the Ryanodine receptor and Cx43 hemichannels. IP3RPEP6 regulates calcium signaling within cells.

Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.