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Results for "

relaxations

" in MCE Product Catalog:

29

Inhibitors & Agonists

6

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-137466
    ARN-21934

    Topoisomerase Cancer
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
  • HY-G0008
    O-Desmethyl Mebeverine alcohol

    Mebeverine metabolite O-desmethyl Mebeverine alcohol

    Adrenergic Receptor Drug Metabolite Metabolic Disease
    O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
  • HY-G0008A
    O-Desmethyl Mebeverine alcohol hydrochloride

    Mebeverine metabolite O-desmethyl Mebeverine alcohol hydrochloride

    Adrenergic Receptor Drug Metabolite Metabolic Disease
    O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
  • HY-19583
    Cicaprost

    ZK 96480

    Prostaglandin Receptor Cancer Cardiovascular Disease
    Cicaprost (ZK 96480) is a prostacyclin receptor (IP) agonist. Cicaprost causes a concentration-dependent relaxation of the artery with an EC50 of 5.8 nM 。
  • HY-139448
    Carboxyebselen

    HOOC-Ebs

    NO Synthase Cardiovascular Disease
    Carboxyebselen (HOOC-Ebs) is a potent and selective inhibitor of endothelial nitric oxide synthase (eNOS).
  • HY-103316
    trans-Ned 19

    Calcium Channel Cardiovascular Disease
    trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
  • HY-101952
    Prostaglandin E2

    PGE2; Dinoprostone

    Prostaglandin Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
  • HY-N0484
    Liensinine

    Autophagy Mitophagy Apoptosis Cancer Cardiovascular Disease
    Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  • HY-B1481
    Isoetharine mesylate

    Isoetarine mesylate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like drug and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
  • HY-N1620
    1-Cinnamoylpyrrolidine

    Others Cardiovascular Disease
    1-Cinnamoylpyrrolidine (Compound 3), a crude extract prepared from Piper caninum, is a DNA strand scission agent, induces the relaxation of supercoiled pBR322 plasmid DNA. 1-Cinnamoylpyrrolidine (Compound 4) inhibits platelet aggregation induced by PAF with an IC50 of 37.3 μM.
  • HY-107416
    RHC 80267

    U-57908

    Acyltransferase mAChR COX Phospholipase Metabolic Disease Neurological Disease
    RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
  • HY-134004
    Pentoxyverine

    Carbetapentane

    Sigma Receptor Neurological Disease
    Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
  • HY-101952S1
    Prostaglandin E2-d9

    PGE2-d9; Dinoprostone-d9

    Prostaglandin Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    Prostaglandin E2-d9 (PGE2-d9) is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
  • HY-N0485
    Liensinine Diperchlorate

    Autophagy Mitophagy Cardiovascular Disease
    Liensinine Diperchlor​ate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlor​ate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlor​ate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-101952S
    Prostaglandin E2-d4

    PGE2-d4; Dinoprostone-d4

    Prostaglandin Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    Prostaglandin E2-d4 (PGE2-d4) is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
  • HY-110137A
    Furamidine

    DB75; NSC 305831

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Cancer Infection Inflammation/Immunology
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
  • HY-110137
    Furamidine dihydrochloride

    DB75 dihydrochloride; NSC 305831 dihydrochloride

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Cancer Infection Inflammation/Immunology
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
  • HY-10061
    Lesogaberan

    AZD-3355

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
  • HY-10061B
    Lesogaberan hydrochloride

    AZD-3355 hydrochloride

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
  • HY-118689
    RA-2

    Potassium Channel Inflammation/Immunology Neurological Disease Cardiovascular Disease
    RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation.
  • HY-101222
    SB-203186 hydrochloride

    5-HT Receptor Neurological Disease Cardiovascular Disease
    SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
  • HY-B1640
    Ethacrynic acid

    Etacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-134004S
    Pentoxyverine-d8

    Sigma Receptor Neurological Disease
    Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
  • HY-10061A
    Lesogaberan napadisylate

    AZD-3355 napadisylate

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    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 calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-W011269
    Eicosapentaenoic Acid sodium

    EPA sodium; Timnodonic acid sodium

    Endogenous Metabolite Histone Demethylase Metabolic Disease Cardiovascular Disease
    Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation.
  • HY-B0660
    Eicosapentaenoic Acid

    EPA; Timnodonic acid

    Endogenous Metabolite Histone Demethylase Neurological Disease Cancer
    Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.
  • HY-150979
    Gd-NMC-3

    Others Cancer
    Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential.