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Ca2 -antagonistic

" in MedChemExpress (MCE) Product Catalog:

95

Inhibitors & Agonists

1

Screening Libraries

9

Peptides

7

Natural
Products

5

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14656S
    Diltiazem-d3 hydrochloride

    		Calcium Channel Cardiovascular Disease
    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-d3 hydrochloride
  • HY-P1479A
    Calmodulin-Dependent Protein Kinase II(290-309) acetate

    		Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) acetate is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II(290-309) acetate
  • HY-103319
    Calmidazolium chloride

    R 24571

    		 Autophagy Calmodulin Neurological Disease Cancer
    Calmidazolium chloride (R 24571) is a calmodulin antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively . Also in anti-cancer research . Calmidazolium binds to calmodulin with a Kd of 3 nM.
    Calmidazolium chloride
  • HY-P1479
    Calmodulin-Dependent Protein Kinase II (290-309)

    		Autophagy CaMK Neurological Disease
    Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II .
    Calmodulin-Dependent Protein Kinase II (290-309)
  • HY-14656S1
    Diltiazem-(acetoxy-d3) (hydrochloride)

    		Isotope-Labeled Compounds Calcium Channel Cardiovascular Disease
    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].
    Diltiazem-(acetoxy-d3) (hydrochloride)
  • HY-119401
    CAY10444
    1 Publications Verification

    BML-241

    		 LPL Receptor Cancer
    CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors .
    CAY10444
  • HY-16952A
    Bepridil hydrochloride hydrate
    5 Publications Verification

    (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
    Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders .
    Bepridil hydrochloride hydrate
  • HY-12962
    NMDA-IN-1

    		iGluR Neurological Disease
    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.
    NMDA-IN-1
  • HY-12542
    Dantrolene
    5+ Cited Publications

    F 368

    		 Calcium Channel Autophagy Neurological Disease Inflammation/Immunology
    Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
    Dantrolene
  • HY-12542A
    Dantrolene sodium hemiheptahydrate
    5+ Cited Publications

    Dantrolene sodium hydrate

    		 Calcium Channel Autophagy Others
    Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
    Dantrolene sodium hemiheptahydrate
  • HY-12542S
    Dantrolene-13C3

    F 368-13C3

    		 Isotope-Labeled Compounds Glutathione Reductase Neurological Disease Inflammation/Immunology
    Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
    Dantrolene-13C3
  • HY-149483
    CVN417

    		nAChR Neurological Disease
    CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
    CVN417
  • HY-N0215S14
    L-Phenylalanine-15N,d8

    (S)-2-Amino-3-phenylpropionic acid-15N,d8

    		 Isotope-Labeled Compounds Calcium Channel iGluR Endogenous Metabolite Metabolic Disease
    L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
    L-Phenylalanine-15N,d8
  • HY-101685
    Iganidipine

    		Calcium Channel Cardiovascular Disease
    Iganidipine is a Ca 2+ antagonist.
    Iganidipine
  • HY-U00354
    CP-060

    		Calcium Channel Cardiovascular Disease
    CP-​060 is a potent Ca 2+ antagonist, inhibits Ca 2+ overload and possesses antioxidant and cardioprotective activities.
    CP-060
  • HY-115745
    Calmodulin antagonist-1

    		Calmodulin Cardiovascular Disease
    Calmodulin antagonist-1 (A-5) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=66 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=560 μM) in a competitive fashion with respect to cyclic GMP .
    Calmodulin <em>antagonist</em>-1
  • HY-100928
    YS 035 hydrochloride

    YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
    YS 035 hydrochloride
  • HY-14656
    Diltiazem hydrochloride
    4 Publications Verification

    CRD-401

    		 Calcium Channel Cardiovascular Disease Cancer
    Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
    Diltiazem hydrochloride
  • HY-117099
    TMB-8

    		Calcium Channel Neurological Disease
    TMB-8 is a novel Ca 2+ antagonist. TMB-8 may exert inhibitory effects in smooth muscle by blocking Ca 2+ release from intracellular bound stores.
    TMB-8
  • HY-U00026
    Semotiadil recemate fumarate

    		Calcium Channel Cardiovascular Disease
    Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca 2+ channel antagonist.
    Semotiadil recemate fumarate
  • HY-U00212
    Aranidipine

    MPC1304

    		 Calcium Channel Cardiovascular Disease
    Aranidipine (MPC1304) is a Ca 2+ channel antagonist with potent and long-lasting antihypertensive effects.
    Aranidipine
  • HY-101669
    TDN345

    		Calcium Channel Neurological Disease
    TDN345 is a Ca 2+ antagonist, used for the treatment of vascular and senile dementia including Alzheimer's disease.
    TDN345
  • HY-19025
    CV-159

    		Calmodulin Inflammation/Immunology
    CV-159 is a unique dihydropyridine Ca 2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
    CV-159
  • HY-137175
    TMBIM6 antagonist-1

    		mTOR Cancer
    TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+ .
    TMBIM6 <em>antagonist</em>-1
  • HY-10388
    TTA-Q6
    1 Publications Verification

    		 Calcium Channel Neurological Disease
    TTA-Q6 is a selective T-type Ca 2+ channel antagonist, which can be used in the research of neurological disease .
    TTA-Q6
  • HY-10171
    NPS-2143 hydrochloride
    10+ Cited Publications

    SB-262470A hydrochloride

    		 CaSR Metabolic Disease
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
    NPS-2143 hydrochloride
  • HY-10007
    NPS-2143
    10+ Cited Publications

    SB-262470A

    		 CaSR Metabolic Disease
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
    NPS-2143
  • HY-19062
    SM-6586

    		Calcium Channel Na+/Ca2+ Exchanger Cardiovascular Disease
    SM-6586 is a calcium channel antagonist and inhibitor of Na +/H + and Na +/Ca 2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
    SM-6586
  • HY-N10754
    Aschantin

    		mTOR Cytochrome P450 Infection Cardiovascular Disease Cancer
    Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
    Aschantin
  • HY-136909
    SR33805

    		Calcium Channel Cardiovascular Disease
    SR33805 is a potent Ca 2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts .
    SR33805
  • HY-120588
    BI 639667

    CCR1 antagonist 8

    		 CCR Inflammation/Immunology Endocrinology
    BI 639667 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist, with an IC50 of 1.8 nM in Ca 2+ flux assay .
    BI 639667
  • HY-14656R
    Diltiazem hydrochloride (Standard)

    CRD-401 (Standard)

    		 Calcium Channel Cardiovascular Disease Cancer
    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 hydrochloride (Standard)
  • HY-121186
    Bevantolol hydrochloride

    		Adrenergic Receptor Calcium Channel Neurological Disease Metabolic Disease
    Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
    Bevantolol hydrochloride
  • HY-120261
    GB-88
    1 Publications Verification

    		 Protease Activated Receptor (PAR) Inflammation/Immunology
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca 2+ release with an IC50 of 2 µM .
    GB-88
  • HY-131041
    Ned-K

    		Calcium Channel Cardiovascular Disease
    Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes .
    Ned-K
  • HY-120691A
    GSK205
    3 Publications Verification

    		 TRP Channel Metabolic Disease Inflammation/Immunology
    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca 2+ influx .
    GSK205
  • HY-10388A
    TTA-Q6(isomer)

    		Calcium Channel Others
    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca 2+ channel antagonist.
    TTA-Q6(isomer)
  • HY-121604
    (Rac)-MEM 1003

    		Calcium Channel Others
    (Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca 2+ channel antagonist and has the potential for Alzheimer’s disease research .
    (Rac)-MEM 1003
  • HY-N0607
    Ginsenoside Ro
    1 Publications Verification

    Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V

    		 Calcium Channel Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V) exhibits a Ca 2+-antagonistic antiplatelet effect with an IC50 of 155  μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
    Ginsenoside Ro
  • HY-133596
    12,14-Dichlorodehydroabietic acid

    		Potassium Channel GABA Receptor Neurological Disease
    12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release .
    12,14-Dichlorodehydroabietic acid
  • HY-131942
    sFTX-3.3

    		Calcium Channel Neurological Disease
    sFTX-3.3 is a Ca 2+ channel antagonist with IC50s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels .
    sFTX-3.3
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
    (-)-Bicuculline methobromide
  • HY-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons .
    (-)-Bicuculline methochloride
  • HY-P1076
    CALP2

    		Calmodulin Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages .
    CALP2
  • HY-157453
    CCR4 antagonist 4

    		CCR Inflammation/Immunology
    CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC50 of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC50: 0.007 μM) and Ca 2+ mobilization (IC50: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research .
    CCR4 <em>antagonist</em> 4
  • HY-P1076A
    CALP2 TFA

    		Calmodulin Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages .
    CALP2 TFA
  • HY-N4267
    Yangambin

    		Calcium Channel Infection Cardiovascular Disease
    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 .
    Yangambin
  • HY-125836
    CCR4 antagonist 2

    		CCR Endocrinology Cancer
    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
    CCR4 <em>antagonist</em> 2
  • HY-B0358A
    Flunarizine dihydrochloride
    3 Publications Verification

    		 Calcium Channel Sodium Channel Dopamine Receptor Neurological Disease
    Flunarizine dihydrochloride is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine dihydrochloride is a D2 dopamine receptor antagonist. Flunarizine dihydrochloride shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
    Flunarizine dihydrochloride
  • HY-B0358
    Flunarizine
    3 Publications Verification
    Flunarizine is a potent dual Na +/Ca 2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects .
    Flunarizine

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