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Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca 2+influx through voltage-dependent calcium channels. Antimycobacterial activity .
Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644 . Bay K 8644 is a L-type Ca 2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca 2+influx through sarcolemmal Ca 2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects .
Farnesyl pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes .
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis) . Nothofagin downregulates NF-κB translocation through blocking calciuminflux. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation .
Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa .
YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders .
Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA .
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels .
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA TFA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA TFA has no effect on L-type or N-type calcium channels .
(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Diltiazem (hydrochloride) (Standard) is the analytical standard of Diltiazem (hydrochloride). This product is intended for research and analytical applications. Diltiazem hydrochloride is a Ca 2+influx inhibitor (slow channel blocker or calcium antagonist).
Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
ITH12575, a CGP37157 derivative, is a potent and selective mNCX blocker. ITH12575 reduces Ca 2+influx through CALHM1 at low micromolar concentrations .
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
CBP-501 is a cell-permeable and calmodulin-binding peptide that enhances the influx of platinum agents into tumor cells and tumor immunogenicity. CBP-501 can be utilized in cancer research .
Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+influx, and DHT-like effects .
OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca 2+influx in Trypanosoma brucei with an IC50 of 0.4 μM .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Aminopterin N-hydroxysuccinimide ester(NHS-methotrexate) is an irreversible
Methotrexate (HY-14519) influx carrier inhibitor. Aminopterin N-hydroxysuccinimide ester can be used for the research of rheumatoid arthritis and a number of cancers (such as acute lymphoblastic leukemia) .
HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+influx and elevate intracellular Ca 2+ in HEK cells .
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca 2+-release channels/ryanodine receptors (RyRs) enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
Mepivacaine (hydrochloride) (Standard) is the analytical standard of Mepivacaine (hydrochloride). This product is intended for research and analytical applications. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
Bekanamycin (Standard) is the analytical standard of Bekanamycin. This product is intended for research and analytical applications. Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels . And (-)-Denudatin B has nonspecific antiplatelet action
MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx .
Gabapentin is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain .
Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research .
Mepivacaine-d3 is the deuterium labeled Mepivacaine. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization[1][2].
(±)-Abscisic acid ((±)-ABA) is an orally active phytohormone. (±)-Abscisic acid induces Ca 2+ channel opening to facilitate the influx of calcium ions and modulates stomatal movement. (±)-Abscisic acid shows anti-inflammatory activity and has the potential for the research of inflammatory bowel disease (IBD) .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+influx, and changes in membrane potential, and is related to channel formation .
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer .
Imperatoxin A TFA is a peptide toxin derived from the venom of the African scorpion Pandinus imperator. Imperatoxin A TFA is a Ca 2+-release channels/ryanodine receptors (RyRs) activator. Imperatoxin A TFA enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Mepivacaine (Standard) is the analytical standard of Mepivacaine. This product is intended for research and analytical applications. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
1,4-Dihydropyridine is an inhibitor for calcium channel, that blocks the L-type calcium channels, reduces the influx of calcium ions into cardiac and vascular smooth muscle cells, and thus reduces the contractility and heart rate of the heart, dilates blood vessels, and lowers blood pressure .
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+influx and Ca 2+ cell overload .
Losigamone (AO-33) is an orally active antiepileptic compound. Losigamone blocks sodium channel. Losigamone stimulates the neuronal chloride channel and enhance chloride influx. Losigamone potentiates GABA-mediated responses and reduces epileptiform activity induced by chloride channel antagonists. Losigamone can be used for epilepsy research .
7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [ 14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux .
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
(+)-Mepivacaine is a racemic isomer of Mepivacaine (HY-B0517), which has analgesic and vasoconstrictive activity. Mepivacaine is an amide type agent that temporarily causes local loss of consciousness. Mepivacaine binds to specific voltage-gated sodium channels on neuronal cell membranes, inhibiting sodium influx and membrane depolarization .
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+influx .
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation .
(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+influx in Trypanosoma brucei, with an IC50 of 0.4 μM .
Gabapentin (Standard) is the analytical standard of Gabapentin. This product is intended for research and analytical applications. Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain .
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer[1][2][3].
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
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 calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Gabapentin-d4 hydrochloride is the deuterium labeled Gabapentin hydrochloride (HY-A0057A). Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells .
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Englerin A (Standard) is the analytical standard of Englerin A. This product is intended for research and analytical applications. Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload .
Deoxypheganomycin D is a specific antimycobacterial inhibitor with activity against the growth of Mycobacterium smegmatis ATCC 607. Deoxypheganomycin D inhibits bacterial growth in a bacteriostatic manner at concentrations up to 7 X 10(-5) M and has no cross-resistance to other antibiotics such as paromomycin, capreomycin, viomycin, streptothricin, kanamycin and streptomycin. Deoxypheganomycin D only partially inhibits the cell growth of M. 607 at 2.8 X 10(-7) M, but has no significant inhibitory effect on DNA, RNA or protein synthesis, while there is a significant reduction in the accumulation of [14C]glycerol-derived radioactive material in the cell wall. Deoxypheganomycin D affects the influx of the amino acid leucine in the presence of 7 X 10(-6) M, while having no effect on the influx of thymidine, whereas the reverse is true for the outflux. The effects of deoxypheganomycin D may be related to cell membrane and specific mycobacterial lipid components .
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .
ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs) .
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].
Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody. Obexelimab works by inhibiting B cell receptor (BCR) mediated calcium influx and promoting the phosphorylation of Fc γ receptor IIb (FcγRIIb), which reduces B cell activation and function, leading to B cell apoptosis. Obexelimab can be used in research for rheumatoid arthritis and systemic lupus erythematosus .
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 calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
Ropivacaine hydrochloride monohydrate is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain?management in vivo .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) .
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane .
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+influx with an IC50 value of 0.43 μM and also inhibits serotonin .
BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Lys-Bradykinin (Kallidin (380-389) (human, porcine, bovine)) tetraacetate, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin tetraacetate, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin tetraacetate involves in vascular regulation, inflammation and pain sensation .
D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co 2+influx in cultured cerebellar granule cells (IC50 ≥ 100 μM) .
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice .
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+influx in macrophages, and inhibits macrophage phagocytosis .
PDDHV is a calcium absorption inducer and may achieve 45Ca 2+influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
Lys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation .
Ropivacaine (Standard) is the analytical standard of Ropivacaine. This product is intended for research and analytical applications. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling .
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]iinflux in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke .
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain?management in vivo .
Ropivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Ropivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease .
Oxatomide (Standard) is the analytical standard of Oxatomide. This product is intended for research and analytical applications. Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+influx with an IC50 value of 0.43 μM and also inhibits serotonin .
(+)-Niguldipine hydrochloride is an antagonist for calcium channel. (+)-Niguldipine hydrochloride produces vasodilation by blocking calcium channels and reducing the transmembrane influx of calcium ions. (+)-Niguldipine hydrochloride inhibits U-46619 (HY-108566)-induced coronary vasoconstriction in guinea pig Langendorff heart with pID50 of 11.37, binds to calcium channel on guinea pig skeletal muscle membrane with Ki of 9.75, and lowers the blood pressure in spontaneously hypertensive rat with pED30 of 7.1. (+)-Niguldipine hydrochloride ameliorates cardiovascular diseases such as hypertension, angina pectoris and arrhythmias .
YM-355179 fumarate is a newly synthesized selective CCR3 antagonist with the potential to inhibit eosinophil-related allergic inflammatory diseases. YM-355179 can effectively inhibit the binding of CCL11 and CCL5 to CCR3-expressing cells, with IC50 values of 7.6 nM and 24 nM respectively. In functional experiments, YM-355179 can inhibit CCL11-induced intracellular Ca(2+) influx, chemotaxis and eosinophil degranulation, IC50 The values are 8.0 nM, 24 nM and 29 nM respectively .
8-Br-7-CH-ADPR (8-Bromo-7-deazaadenosine-5'-O-diphosphoribose) is a specific TRPM2 antagonist that inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel, thereby controlling the influx of cations through the cell membrane channel. 8-Br-7-CH-ADPR can be used to study the role of TRPM2 in pathological processes such as cell death, neurodegenerative diseases, myocardial infarction, and diabetes .
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Anisodine hydrobromide is a neuroprotective compound that interacts with muscarinic receptors (M1-M5) in cerebral ischemic diseases. Anisodine hydrobromide effectively reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine hydrobromide demonstrates concentration-dependent inhibition of calcium ion influx and reactive oxygen species (ROS) levels, elucidating its neuroprotective mechanisms. Anisodine hydrobromide leads to decreased aspartate levels in HM cells during hypoxia, highlighting its effects on neurotransmitter modulation. Anisodine hydrobromide holds promising clinical prospects as a potential therapeutic agent for ischemic brain diseases, warranting further investigation into its mechanisms of action.
PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA TFA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA TFA has no effect on L-type or N-type calcium channels .
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa .
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels .
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca 2+-release channels/ryanodine receptors (RyRs) enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+influx, and changes in membrane potential, and is related to channel formation .
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
Imperatoxin A TFA is a peptide toxin derived from the venom of the African scorpion Pandinus imperator. Imperatoxin A TFA is a Ca 2+-release channels/ryanodine receptors (RyRs) activator. Imperatoxin A TFA enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
Lys-Bradykinin (Kallidin (380-389) (human, porcine, bovine)) tetraacetate, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin tetraacetate, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin tetraacetate involves in vascular regulation, inflammation and pain sensation .
Lys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation .
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease .
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody. Obexelimab works by inhibiting B cell receptor (BCR) mediated calcium influx and promoting the phosphorylation of Fc γ receptor IIb (FcγRIIb), which reduces B cell activation and function, leading to B cell apoptosis. Obexelimab can be used in research for rheumatoid arthritis and systemic lupus erythematosus .
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca 2+influx through voltage-dependent calcium channels. Antimycobacterial activity .
Farnesyl pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA .
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+influx, and DHT-like effects .
Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis) . Nothofagin downregulates NF-κB translocation through blocking calciuminflux. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation .
(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Bekanamycin (Standard) is the analytical standard of Bekanamycin. This product is intended for research and analytical applications. Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels . And (-)-Denudatin B has nonspecific antiplatelet action
(±)-Abscisic acid ((±)-ABA) is an orally active phytohormone. (±)-Abscisic acid induces Ca 2+ channel opening to facilitate the influx of calcium ions and modulates stomatal movement. (±)-Abscisic acid shows anti-inflammatory activity and has the potential for the research of inflammatory bowel disease (IBD) .
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+influx and Ca 2+ cell overload .
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation .
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Englerin A (Standard) is the analytical standard of Englerin A. This product is intended for research and analytical applications. Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload .
Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
FYN Protein, Human (Biotinylated, sf9, His, Flag, Avi) is the recombinant human-derived FYN, expressed by Sf9 insect cells , with Avi, His, Flag labeled tag. The total length of FYN Protein, Human (Biotinylated, sf9, His, Flag, Avi) is 537 a.a.,
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Mepivacaine-d3 is the deuterium labeled Mepivacaine. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization[1][2].
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer[1][2][3].
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine 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 calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Gabapentin-d4 hydrochloride is the deuterium labeled Gabapentin hydrochloride (HY-A0057A). Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, 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 calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain?management in vivo .
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