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Results for "

H3R

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112219A
    H3R antagonist 1 hydrochloride

    		Histamine Receptor Inflammation/Immunology Endocrinology
    H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
    H3R antagonist 1 hydrochloride
  • HY-112219
    H3R antagonist 1

    		Histamine Receptor Inflammation/Immunology Endocrinology
    H3R-IN-1 is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.
    H3R antagonist 1
  • HY-120124
    Samelisant

    SUVN-G3031

    		 Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
    Samelisant
  • HY-12190
    JNJ-5207852

    		Histamine Receptor Neurological Disease Endocrinology
    JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
    JNJ-5207852
  • HY-162812
    H3R antagonist 4

    		Apoptosis Cholinesterase (ChE) Tau Protein Ferroptosis Histamine Receptor Neurological Disease
    H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
    H3R antagonist 4
  • HY-146383
    H3R antagonist 2

    		Histamine Receptor Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .
    H3R antagonist 2
  • HY-126748
    VUF14862

    		Others Others
    VUF14862 is a robust and fatigue-resistant photoswitchable GPCR antagonist that exhibits over a 10-fold increase in H3R binding affinity upon illumination at 360 nm. VUF14862 can be utilized for spatiotemporal studies of H3R signaling .
    VUF14862
  • HY-161333
    ADS031

    		Histamine Receptor Inflammation/Immunology
    ADS031, a histamine H3R antagonist, displays 12.5 nM affinity at the hH3R and the highest inhibitory activity against AChE (IC50 = 1.537 μM) .
    ADS031
  • HY-122171
    A-317920

    		Histamine Receptor Neurological Disease
    A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
    A-317920
  • HY-122608
    Samelisant free base

    SUVN-G3031 free base

    		 Histamine Receptor Neurological Disease
    Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
    Samelisant free base
  • HY-12190A
    JNJ-5207852 dihydrochloride

    		Histamine Receptor Neurological Disease
    JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
    JNJ-5207852 dihydrochloride
  • HY-109968A
    Irdabisant hydrochloride

    CEP-26401 hydrochloride

    		 Histamine Receptor Neurological Disease
    Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
    Irdabisant hydrochloride
  • HY-109968
    Irdabisant

    CEP-26401

    		 Histamine Receptor Neurological Disease
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
    Irdabisant
  • HY-128656
    LML134

    		Histamine Receptor Neurological Disease Endocrinology
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
    LML134
  • HY-12195
    ABT-239
    2 Publications Verification

    		 Histamine Receptor TRP Channel Neurological Disease Endocrinology
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 
    ABT-239
  • HY-101198
    Clobenpropit dihydrobromide

    		Histamine Receptor Apoptosis Neurological Disease Cancer
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis [3].
    Clobenpropit dihydrobromide
  • HY-19881
    ABT-288

    		Histamine Receptor Neurological Disease
    ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has Ki values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research. .
    ABT-288
  • HY-108058A
    Immethridine dihydrobromide

    		Histamine Receptor Inflammation/Immunology
    Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
    Immethridine dihydrobromide
  • HY-111501
    H4R antagonist 1

    		Histamine Receptor Inflammation/Immunology Endocrinology
    H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
    H4R antagonist 1
  • HY-146035
    AChE-IN-14

    		Cholinesterase (ChE) Histamine Receptor Neurological Disease
    AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease .
    AChE-IN-14
  • HY-169156
    HDAC6-IN-49

    		HDAC Monoamine Oxidase Cholinesterase (ChE) Histamine Receptor 5-HT Receptor Neurological Disease
    HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models .
    HDAC6-IN-49
  • HY-100360
    MS049

    		Histone Methyltransferase Cancer
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
    MS049
  • HY-100360A
    MS049 dihydrochloride

    		Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
    MS049 dihydrochloride

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