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Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calciumchannel blocker with moderate selectivity for T-type Ca 2+channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively) .
Magnesium sulfate is a calcium antagonist and a potent L-typecalciumchannel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia .
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Pinaverium bromide is an L-typecalciumchannel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients .
Clevidipine is a selective, short-acting L-typecalciumchannel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calciumchannels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury .
Azelnidipine (CS 905) is a dihydropyridine calciumchannel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-typecalciumchannel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .
Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-typecalciumchannel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride 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 hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Fluspirilene is a non-competitive antagonist of L-typecalciumchannels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.
Cinnarizine is an orally active, effective and selective inhibitor of L-typecalciumchannelCav1.3 with an IC50 of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-typecalciumchannels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases .
Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-typecalciumchannels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
Etripamil (MSP-2017) is a short-acting, L-typecalcium-channel antagonist. Etripamil inhibits calcium influx through slow calciumchannels, thereby slowing AV node conduction and prolonging the AV node refractory period. Etripamil increases heart rate and decreases systolic blood pressure. Etripamil can be used in the study of paroxysmal supraventricular tachycardia (PSVT) .
Magnesium sulfate, for cell culture is a bioreagent. Magnesium sulfate is a calcium antagonist and a potent L-typecalciumchannel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia .
Drotaverine hydrochloride is a type4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calciumchannel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Fendiline, a diphenylalkylamine type of antianginal agent, is an L-typecalciumchannel 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) .
Levamlodipine ((S)-Amlodipine; Levoamlodipin) is an orally active L-typecalciumchannel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine 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 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 exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine 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 can be used in research related to hypertension and atherosclerosis .
Mibefradil (Ro 40-5967) is a calciumchannel blocker with moderate selectivity for T-type Ca 2+channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively .
VU6032735 is a potent and subtype-selective sperm-specific potassium channel 3 (SLO3) inhibitor with IC50 values of 165 nM (hSLO3) and 730 nM (mSLO3). VU6032735 also inhibits sodium channel and L-typecalciumchannel VU6032735 can sustain high tissue exposure in the fertilized oviduct. VU6032735 can be used for the research of contraception .
(R)-Nimodipine ((R)-BAY-e 9736) is an orally active, blood-brain barrier-permeable L-typecalciumchannel blocker with an IC50 of 5 nM. (R)-Nimodipine inhibits corticosterone release by blocking calciumchannels on the hypothalamic-pituitary-adrenal axis, thereby reversing immobilization stress-induced memory impairment and behavioral abnormalities. (R)-Nimodipine is widely used in studies related to aneurysmal subarachnoid hemorrhage, cerebral ischemia, epilepsy, age-related degenerative neurological diseases, and alcohol intoxication .
Pranidipine (OPC-13340) is an orally active L-type voltage-dependent calciumchannel (L-VDCC) blocker with a Ki value of 0.16 nM. Pranidipine inhibits calcium-induced contraction, suppresses slow-response action potentials, shortens action potential duration, reduces systolic and diastolic blood pressure, and exerts vasodilatory effects. Pranidipine enhances its vasodilatory effect by blocking NO decomposition. Pranidipine can be used in research related to essential hypertension, angina pectoris, myocardial infarction, and dilated cardiomyopathy .
Ethaverine hydrochloride, a derivative of papaverine, inhibits cardiac L-typecalciumchannel. Ethaverine hydrochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine hydrochloride can be used for research of peripheral vascular disease .
Nemadipine-A is a specific inhibitor of the EGL-19 L-typeCa 2+channel . Nemadipine-A, a cell-permeable L-typecalciumchannel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand .
Fendiline (hydrochloride) (Standard) is the analytical standard of Fendiline (hydrochloride). This product is intended for research and analytical applications. Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-typecalciumchannel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride 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 hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
Didrovaltrate (Didrovaltratum) is an L-typecalciumchannel blocker, ROS scavenger, autophagy enhancer, and lipid accumulation inhibitor. Didrovaltrate blocks L-typecalcium currents in a concentration-dependent manner, shifts the current-voltage curve upward, modulates steady-state inactivation kinetics, and inhibits the nuclear translocation of glucocorticoid receptors. Didrovaltrate reduces ROS levels, downregulates the expression of muscle atrophy-related genes, enhances autophagy via lipophagy, and decreases Oleic acid-induced lipid accumulation. Didrovaltrate exhibits cytotoxic activity against cancer cells. Didrovaltrate can be used in research related to skeletal muscle atrophy, non-alcoholic fatty liver disease, breast cancer, lung cancer, gastric cancer, and prostate cancer .
N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calciumchannels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-typecalciumchannels .
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calciumchannels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12 .
MONIRO-1 is a T-type and N-typecalciumchannel blocker with IC50 values of 34, 3.3, 1.7 and 7.2 µM against hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively. MONIRO-1 has low activity against L-typecalciumchannels. MONIRO-1 can be used for the study of pain and epilepsy .
Felodipine 3,5-Dimethyl Ester is a aryldihydropyridine derivatives for use as mineralocorticoid receptor modulator and voltage-dependent L-typecalciumchannel CaV1.2 inhibitor .
Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calciumchannel, especially L-typecalciumchannel .
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer .
SL-870495 is a calcium antagonist targeting L-typecalciumchannels. SL-870495 is promising for research of cardiovascular diseases such as hypertension and angina pectoris .
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
HM12 is a covalent inhibitor of L-/T-typecalciumchannels. HM12 can strongly inhibit the Cav1.2 (L-type) and Cav3.2 (T-type) calciumchannels, and has selectivity for the N-typechannels. HM12 produces an irreversible inhibition that persisted after washout. HM12 can be used to study diseases such as hypertension, pain, epilepsy, etc .
Pinaverium bromide-d4 is deuterium labeled Pinaverium bromide. Pinaverium bromide is an L-typecalciumchannel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients .
Pinaverium bromide (Standard) is the analytical standard of Pinaverium bromide. This product is intended for research and analytical applications. Pinaverium bromide is an L-typecalciumchannel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients .
(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-typecalciumchannels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp) .
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Etripamil (MSP-2017) hydrochloride is a short-acting, L-typecalciumchannel antagonist that can be used in the study of paroxysmal supraventricular tachycardia (PSVT). Etripamil hydrochloride inhibits calcium influx through slow calciumchannels, thereby slowing atrioventricular node conduction and prolonging the atrioventricular node refractory period.
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Amlodipine (Standard) is the analytical standard of Amlodipine. This product is intended for research and analytical applications. Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Sornidipine is a calciumchannel blocker. Sornidipine also reduces neurogenic inflammation. Sornidipine reduces the inflow of calcium ions into cells by blocking L-typecalciumchannels, thereby reducing the contraction of vascular smooth muscle, leading to vasodilation and decreased blood pressure. Sornidipine can be used to study the cardiovascular system especially in hypertension and related cardiovascular diseases .
Amlodipine (maleate) (Standard) is the analytical standard of Amlodipine (maleate). This product is intended for research and analytical applications. Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Amlodipine (maleate) (Standard) is the analytical standard of Amlodipine (maleate). This product is intended for research and analytical applications. Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-typecalciumchannels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
AJG049 free base is a calciumchannel (Ca 2+channel) antagonist. AJG049 free base regulates vascular relaxation, reduces cardiac load, and improves cardiac perfusion by binding to the binding site of L-typecalciumchannels, specifically Diltiazem (HY-B0632). AJG049 free base can be used in cardiovascular disease research .
SB-237376 is a blocker of potassium and calciumchannels. SB-237376 inhibits the rapidly activating delayed rectifier potassium current I(Kr) (IC50: 0.42 μM) and blocks the L-typecalcium current I(Ca,L) at high concentrations .
Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-typecalciumchannels .
Amlodipine (besylate) (Standard) is the analytical standard of Amlodipine (besylate). This product is intended for research and analytical applications. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Azelnidipine (Standard) is the analytical standard of Azelnidipine. This product is intended for research and analytical applications. Azelnidipine (CS 905; Calblock) is a dihydropyridine derivative, an L-typecalciumchannel blocker, and can fight hypertension.
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Elgodipine (IQB-875 free base) is an orally active dihydropyridine calcium antagonist and an antianginal compound. Elgodipine inhibits both T- and L-typecalciumchannels (IC50: 32 and 2.3 nM). Elgodipine lowers systemic vascular resistance and improves systolic cardiac function .
Diltiazem malate is a potent and orally active L-typecalciumchannel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris .
FluoBar1 is an imaging fluorescence probe modified by a barbiturate ligand with fluorescent coumarin. FluoBar1 can monitor L-type voltage-gated calciumchannels (LTCC) in living cells in real time for the study of neurological diseases .
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-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
L803 is a selective Somatostatin Receptor Subtype 4 (SST4) agonist. L803 inhibits L-typecalciumchannel currents (ICa). L803 is promising for research of retinal ganglion cell (RGC) degenerative diseases (e.g., glaucoma) .
Ethaverine (hydrochloride) (Standard) is the analytical standard of Ethaverine (hydrochloride). This product is intended for research and analytical applications. Ethaverine hydrochloride, a derivative of papaverine, inhibits cardiac L-typecalciumchannel. Ethaverine hydrochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine hydrochloride can be used for research of peripheral vascular disease .
Ethaverine (hydrochloride) (Standard) is the analytical standard of Ethaverine (hydrochloride). This product is intended for research and analytical applications. Ethaverine hydrochloride, a derivative of papaverine, inhibits cardiac L-typecalciumchannel. Ethaverine hydrochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine hydrochloride can be used for research of peripheral vascular disease .
Nisoldipine-d4 (BAY-k 5552-d4) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM .
Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM .
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calciumchannel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects .
Drotaverine (hydrochloride) (Standard) is the analytical standard of Drotaverine (hydrochloride). This product is intended for research and analytical applications. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calciumchannel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
N-Desalkylflurazepam (Standard) is the analytical standard of N-Desalkylflurazepam. This product is intended for research and analytical applications. N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calciumchannels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
N-Desalkylflurazepam-d4 is a deuterated labeled N-Desalkylflurazepam (HY-106454). N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calciumchannels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calciumchannel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
AH-1058 is a newly synthesized antiarrhythmic agent that exhibits significant antiarrhythmic activity by delaying premature ventricular complexes and ventricular fibrillation in experimental arrhythmia models. AH-1058 effectively inhibits both ventricular tachycardia and ventricular fibrillation in the reperfusion-induced arrhythmia model in rats. AH-1058 demonstrates potent calciumchannel-blocking effects, suppressing L-type Ca2+ currents in isolated cardiomyocytes.
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic 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 calciumchannel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
SB-237376 (free base) is a potassium and calciumchannel blocker. SB-237376 (free base) can inhibit the rapidly activating delayed rectifier potassium current I(Kr) (IC50 is 0.42 μM), and at high concentrations, it blocks the L-typecalcium current I(Ca,L). In the rabbit ventricular model, SB-237376 (free base) can induce early afterdepolarizations (EADs) at a concentration of 3 µM. Compared to other IKr inhibitors such as dl-sotalol, SB-237376 has a lower proarrhythmic risk. SB-237376 (free base) holds potential for research in the field of arrhythmia-related diseases .
RCC-36 hydrochloride is an L-typecalciumchannel inhibitor and competitive muscarinic receptor antagonist. RCC-36 hydrochloride inhibits L-typecalcium currents in voltage- and concentration-dependent fashion with no effect on cardiac K + currents. RCC-36 hydrochloride suppresses maximum acetylcholine-induced contractile responses, inhibits detrusor muscle contractions induced by potassium chloride, calcium chloride, and electric field stimulation, including atropine-resistant contractions. RCC-36 hydrochloride can be used for the research of urinary frequency, urinary incontinence, and bladder overactivity .
Calciseptine TFA, a polypeptide found in black mamba venom, is a selcetive Cav1.2L-typecalciumchannel inhibitor with an IC50 of 92 nM. Calciseptine TFA binds to the pore domain shoulder at repeats III and IV of Cav1.2, stabilizing an inactivated conformation. Calciseptine TFA exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine TFA can be used for the research of cardiovascular diseases .
CPU-228 is a complex class III antiarrhythmic agent. CPU-228 concentration-dependently blocks the activities of the rapid component 50 of the delayed rectifier potassium channel (IKr) and the L-typecalciumchannel (ICa,L), with an IC50 value of 0.909 μM for ICa,L current. CPU-228 produces negative inotropic effects and induces mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atria. CPU-228 reduces the incidence of torsades de pointes (TDP) in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats. CPU-228 can be used in studies related to torsades de pointes .
Amlodipine orotate, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine orotate can be used for the research of high blood pressure and cancer .
A-278637 is a selective KATP channel opening agent with an EC50 of 102 nM. A-278637 does not interact with other ion channels, including L-typecalciumchannels or other neurotransmitter receptor systems. A-278637 possesses a greater functional selectivity for urinary bladder versus vascular smooth muscle in vivo. A-278637 can be used for the study of overactive bladder .
Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-typecalciumchannel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-typecalciumchannels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Efonidipine (NZ-105) is an orally active dual L-type and T-typecalciumchannel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-typecalciumchannels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Azimilide (NE-10064) is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide blocked HERGchannel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide also inhibits L-typecalcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide can be used for the study of atrial fibrillation and ventricular fibrillation .
Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERGchannel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-typecalcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation .
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 calciumchannel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-typecalciumchannel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-typecalciumchannel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-typecalciumchannel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research .
Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-typecalciumchannels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-typecalciumchannel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-typecalciumchannels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
PAF antagonist-1 is a platelet activating factor (PAF) receptor antagonist with a target Ki of 69 nM. PAF antagonist-1 inhibits PAF binding and displays enhanced affinity at A1, A2a, and A3 adenosine receptor subtypes compared to related dihydropyridine analogs with smaller ester groups. PAF antagonist-1 can be used for cardiovascular disorders, especially hypertension and coronary heart disease .
BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-typecalciumchannel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease .
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) TFA is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calciumchannel inhibitor. ω-Hexatoxin-Hv1a TFA blocks L-type voltage-dependent Ca 2+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 TFA 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 TFA is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons .
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calciumchannel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca 2+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 .
Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERGchannel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-typecalcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation .
Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-typecalciumchannels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses .
Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-typecalciumchannel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-typecalciumchannels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Calciseptine is a natural polypeptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis). Calciseptine is a highly effective and selective blocker of the L-type channel of the Cav1.2 subtype, with an IC50 value of 92 nM. Calciseptine has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine can be used for research on cardiovascular diseases[1].
Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β1 adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β1 receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride has little effect on cardiac ion channels (such as L-typecalcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury .
Landiolol (ONO1101) is a highly selective, ultra-short-acting competitive inhibitor of β1 adrenergic receptors. Landiolol specifically blocks cardiac β1 receptors, reducing heart rate and myocardial oxygen consumption. Landiolol inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol has little effect on cardiac ion channels (such as L-typecalcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury .
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca 2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .
5-Hydroxyindole (Standard) is the analytical standard of 5-Hydroxyindole (HY-W001160). This product is intended for research and analytical applications. 5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-typecalciumchannels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
Landiolol (ONO1101) hydrochloride (Standard) is the analytical standard of Landiolol hydrochloride (HY-100607A). This product is intended for research and analytical applications. Landiolol (ONO1101) hydrochloride is a highly selective, ultra-short-acting competitive inhibitor of β1 adrenergic receptors. Landiolol hydrochloride specifically blocks cardiac β1 receptors, reducing heart rate and myocardial oxygen consumption. Landiolol hydrochloride inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol hydrochloride has little effect on cardiac ion channels (such as L-typecalcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol hydrochloride can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury .
ONO-2921 is an orally active and selective N-typecalciumchannel blocker. ONO-2921 functionally blocks N-typecalciumchannels. 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 .
Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrochloride is an orally active L-typecalciumchannel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine hydrochloride 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 hydrochloride 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 hydrochloride exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine hydrochloride 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 hydrochloride can be used in research related to hypertension and atherosclerosis .
Levamlodipine besylate Hemipentahydrate is an orally active L-typecalciumchannel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate Hemipentahydrate 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 Hemipentahydrate 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 Hemipentahydrate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate Hemipentahydrate 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 Hemipentahydrate can be used in research related to hypertension and atherosclerosis .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine; Levoamlodipin) is an orally active L-typecalciumchannel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine 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 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 exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine 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 can be used in research related to hypertension and atherosclerosis .
Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrobromide is an orally active L-typecalciumchannel 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 .
Levamlodipine ((S)-Amlodipine; Levoamlodipin) besylate is an orally active L-typecalciumchannel 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 .
Psoralenoside is an orally active benzofuran glycoside. Psoralenoside is isolated from the fruits of Psoralea corylifolia. As a metabolite precursor, Psoralenoside undergoes deglycosylation by intestinal flora to form Psoralen (HY-N0053). Psoralenoside is applicable to research related to cancer and bacterial infections .
FluoBar1 is an imaging fluorescence probe modified by a barbiturate ligand with fluorescent coumarin. FluoBar1 can monitor L-type voltage-gated calciumchannels (LTCC) in living cells in real time for the study of neurological diseases .
Magnesium sulfate is a calcium antagonist and a potent L-typecalciumchannel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia .
Magnesium sulfate, for cell culture is a bioreagent. Magnesium sulfate is a calcium antagonist and a potent L-typecalciumchannel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia .
Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-typecalciumchannel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-typecalciumchannels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca 2+channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ in cerebral isolated nerve endings with an IC50 of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-typecalciumchannels .
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calciumchannel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca 2+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 .
Calciseptine is a natural polypeptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis). Calciseptine is a highly effective and selective blocker of the L-type channel of the Cav1.2 subtype, with an IC50 value of 92 nM. Calciseptine has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine can be used for research on cardiovascular diseases[1].
Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calciumchannel, especially L-typecalciumchannel .
L803 is a selective Somatostatin Receptor Subtype 4 (SST4) agonist. L803 inhibits L-typecalciumchannel currents (ICa). L803 is promising for research of retinal ganglion cell (RGC) degenerative diseases (e.g., glaucoma) .
Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-typecalciumchannel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
Calciseptine TFA, a polypeptide found in black mamba venom, is a selcetive Cav1.2L-typecalciumchannel inhibitor with an IC50 of 92 nM. Calciseptine TFA binds to the pore domain shoulder at repeats III and IV of Cav1.2, stabilizing an inactivated conformation. Calciseptine TFA exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine TFA can be used for the research of cardiovascular diseases .
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) TFA is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calciumchannel inhibitor. ω-Hexatoxin-Hv1a TFA blocks L-type voltage-dependent Ca 2+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 TFA 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 TFA is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons .
5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-typecalciumchannels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-typecalciumchannels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses .
Didrovaltrate (Didrovaltratum) is an L-typecalciumchannel blocker, ROS scavenger, autophagy enhancer, and lipid accumulation inhibitor. Didrovaltrate blocks L-typecalcium currents in a concentration-dependent manner, shifts the current-voltage curve upward, modulates steady-state inactivation kinetics, and inhibits the nuclear translocation of glucocorticoid receptors. Didrovaltrate reduces ROS levels, downregulates the expression of muscle atrophy-related genes, enhances autophagy via lipophagy, and decreases Oleic acid-induced lipid accumulation. Didrovaltrate exhibits cytotoxic activity against cancer cells. Didrovaltrate can be used in research related to skeletal muscle atrophy, non-alcoholic fatty liver disease, breast cancer, lung cancer, gastric cancer, and prostate cancer .
Psoralenoside is an orally active benzofuran glycoside. Psoralenoside is isolated from the fruits of Psoralea corylifolia. As a metabolite precursor, Psoralenoside undergoes deglycosylation by intestinal flora to form Psoralen (HY-N0053). Psoralenoside is applicable to research related to cancer and bacterial infections .
Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calciumchannel, especially L-typecalciumchannel .
5-Hydroxyindole (Standard) is the analytical standard of 5-Hydroxyindole (HY-W001160). This product is intended for research and analytical applications. 5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-typecalciumchannels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
The CACNA1C protein is the alpha-1C subunit of voltage-gated calcium channels that generate L-type calcium currents that are critical for calcium influx and sarcoplasmic release. Its role in excitation-contraction coupling is critical for cardiac development, rhythm regulation, and smooth muscle cell contraction. CACNA1C Protein, Pig (Cell-Free, His) is the recombinant pig-derived CACNA1C protein, expressed by E. coli Cell-free , with N-10*His labeled tag.
The CACNA2D1 protein, particularly its α-2/δ subunit, plays a key role in regulating calcium current density and activation/deactivation kinetics of voltage-dependent calcium channels. It contributes to excitation-contraction coupling, coordinating cellular processes. CACNA2D1 Protein, Human (His-SUMO) is the recombinant human-derived CACNA2D1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.
Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Pinaverium bromide-d4 is deuterium labeled Pinaverium bromide. Pinaverium bromide is an L-typecalciumchannel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients .
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calciumchannel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calciumchannel blocker, works by blocking the voltage-dependent L-typecalciumchannels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Nisoldipine-d4 (BAY-k 5552-d4) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM .
Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calciumchannel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM .
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-typecalciumchannel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-typecalciumchannel blocker that acts on smooth muscle calciumchannels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calciumchannel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects .
N-Desalkylflurazepam-d4 is a deuterated labeled N-Desalkylflurazepam (HY-106454). N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calciumchannels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+channels and large-conductance calcium-activated potassium channels (BKCachannels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERGchannel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-typecalcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine; Levoamlodipin) is an orally active L-typecalciumchannel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine 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 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 exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine 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 can be used in research related to hypertension and atherosclerosis .
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-typecalciumchannel blocker and a P-glycoprotein (P-gp) function inhibitor .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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