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functional selectivity

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76

Inhibitors & Agonists

1

Screening Libraries

3

Biochemical Assay Reagents

3

Peptides

4

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148258

    NOD-like Receptor (NLR) Interleukin Related Caspase Inflammation/Immunology
    GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation .
    GDC-2394
  • HY-103475

    GABA Receptor Neurological Disease
    GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction .
    GS39783
  • HY-14900

    GRC-10693

    Cannabinoid Receptor Inflammation/Immunology
    Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
    Tedalinab
  • HY-16996A
    BD-1047 dihydrobromide
    Maximum Cited Publications
    6 Publications Verification

    Sigma Receptor Neurological Disease
    BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia .
    BD-1047 dihydrobromide
  • HY-110132

    CCR Inflammation/Immunology
    JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2 .
    JNJ-27141491
  • HY-B1613

    Dopamine Receptor Neurological Disease Metabolic Disease
    Clebopride is a selective dopamine receptor antagonist. Clebopride can be used in the study of functional gastrointestinal disorders .
    Clebopride
  • HY-W017604

    m-Aminophenylboronic acid

    Biochemical Assay Reagents Others
    3-Aminophenylboronic acid (m-Aminophenylboronic acid) functionalized copper nanoclusters can rapidly, selectively and sensitively detect glycoproteins .
    3-Aminophenylboronic acid
  • HY-161105

    5-HT Receptor Others
    FPIP is a selectivity agonist of 5-HT1A with a functional potency (pEC50=8.92) .
    FPIP
  • HY-112426

    GABA Receptor Neurological Disease
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM .
    LAU159
  • HY-128126

    Potassium Channel Cardiovascular Disease
    B-TPMF is a selective inhibitor of the KCa2.1 channel, with an IC50 of 30 nM, and it has a competitive functional interaction with CM-TPMF .
    B-TPMF
  • HY-101336

    RS-17053

    Adrenergic Receptor Metabolic Disease Endocrinology
    RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
    RS 17053 hydrochloride
  • HY-126346

    GPR84 Inflammation/Immunology
    DL-175 (compound 13) is a selective GPR84 agonist with biased agonistic activity. DL-175 can selectively activate functional responses in immune cells and induce enhanced chemotaxis and phagocytosis of human bone marrow cells. DL-175 is a potential chemical probe .
    DL-175
  • HY-106432A

    SB-202026 hydrochloride; Memric hydrochloride

    mAChR Neurological Disease
    Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .
    Sabcomeline hydrochloride
  • HY-106432

    SB-202026; Memric

    mAChR Neurological Disease
    Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .
    Sabcomeline
  • HY-18760

    mGluR Neurological Disease
    LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively) .
    LY2812223
  • HY-16996

    Sigma Receptor Neurological Disease
    BD-1047 is a selective functional antagonist of sigma receptors. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .
    BD-1047
  • HY-120792

    mAChR Others
    DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
    DAU 5884
  • HY-10013
    Taranabant
    2 Publications Verification

    MK-0364

    Cannabinoid Receptor Metabolic Disease
    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
    Taranabant
  • HY-151682

    ADC Linker Others
    H-L-Lys(Norbornene-methoxycarbonyl)-OH, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH can be used for the mild and selective modification of proteins in a copper-free click reaction .
    H-L-Lys(Norbornene-methoxycarbonyl)-OH
  • HY-151682A

    ADC Linker Others
    H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride, a norbornene-derivatized lysine, can be click-functionalized. H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride can be used for the mild and selective modification of proteins in a copper-free click reaction .
    H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride
  • HY-112612

    GPR88 Neurological Disease
    RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats .
    RTI-13951-33
  • HY-112612A
    RTI-13951-33 hydrochloride
    2 Publications Verification

    GPR88 Neurological Disease
    RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats .
    RTI-13951-33 hydrochloride
  • HY-114231

    ELX-02; NB-124

    Others Others
    Exaluren (ELX-02) is an synthetic eukaryotic ribosome-selective glycoside that induces read through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren is used for the research of cystic fibrosis caused by nonsense mutations .
    Exaluren
  • HY-157468

    Others Others
    (R)-ELX-02, also referred to as NB-124, is an eukaryotic ribosomal selective glycoside (ERSG) engineered to enhance read-through activity in patients with nonsense mutations, facilitating the generation of adequate levels of full-length functional protein.
    (R)-ELX-02
  • HY-125096

    Glucocorticoid Receptor Metabolic Disease Inflammation/Immunology
    C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation .
    C108297
  • HY-114996
    ADAMTS-5 Inhibitor
    3 Publications Verification

    ADAMTS Inflammation/Immunology
    ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1) .
    ADAMTS-5 Inhibitor
  • HY-107748A

    5'-GNTI TFA

    Endogenous Metabolite Neurological Disease
    5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .
    5'-Guanidinonaltrindole TFA
  • HY-103416
    A-77636 hydrochloride
    1 Publications Verification

    Dopamine Receptor Neurological Disease
    A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor .
    A-77636 hydrochloride
  • HY-164819

    Dopamine Receptor Neurological Disease
    UNC10099984A (Compound 6) is a functionally selective ligand for the dopamine D2 receptor, with a Ki value of 4.6 nM and an EC50 value of 6.2 nM for β-arrestin. UNC10099984A can be used for research into central nervous system disorders related to the D2 receptor .
    UNC10099984A
  • HY-121467A

    Z-338; YM443

    Cholinesterase (ChE) Others Metabolic Disease Inflammation/Immunology
    Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
    Acotiamide hydrochloride
  • HY-121467

    Z-338 free base; YM443 free base

    Cholinesterase (ChE) Metabolic Disease Inflammation/Immunology
    Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
    Acotiamide
  • HY-111385
    UNC9994 hydrochloride
    1 Publications Verification

    Dopamine Receptor 5-HT Receptor Arrestin Neurological Disease
    UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
    UNC9994 hydrochloride
  • HY-117862

    Prostaglandin Receptor Inflammation/Immunology
    TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guinea pig bronchial asthma models .
    TASP0412098
  • HY-19618

    HDAC HIV Apoptosis Infection Metabolic Disease
    BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency .
    BRD3308
  • HY-D0976

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
    NF279
  • HY-120820

    5-HT Receptor Neurological Disease
    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 .
    LY320954
  • HY-115487

    Prostaglandin Receptor Inflammation/Immunology Cancer
    MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research .
    MF-766
  • HY-167862

    Endogenous Metabolite Neurological Disease
    UCM-05194 is a selective LPA1 receptor agonist with activity to improve neuropathic pain. UCM-05194 is a LPA1 agonist that exhibits potent and selective properties in its pharmacologically similar properties. UCM-05194 triggers LPA1-mediated cellular effects and leads to internalization of the receptor, resulting in functional inactivation in primary sensory neurons. UCM-05194 effectively reduces pain perception in in vivo models. UCM-05194 can be used to conduct research on progressive systemic diseases .
    UCM-05194
  • HY-18664
    PFI-4
    1 Publications Verification

    Epigenetic Reader Domain Cancer
    PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions .
    PFI-4
  • HY-B2155

    Cholinesterase (ChE) Metabolic Disease Inflammation/Immunology
    Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
    Acotiamide monohydrochloride trihydrate
  • HY-14495

    EX-1314

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents .
    BMS-604992
  • HY-14495B

    EX-1314 dihydrochloride

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents .
    BMS-604992 dihydrochloride
  • HY-126220

    Fluorescent Dye Others
    KMG-301AM is the acetoxy methyl esterified form of KMG-301. KMG-301AM successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg 2+-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrial membrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrial membrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg 2+ transport across the mitochondrial membrane in the early phases of a cellular model .
    KMG-301AM
  • HY-13499

    CCR2 antagonist 5

    CCR Inflammation/Immunology
    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 .
    JNJ-41443532
  • HY-126220A

    Fluorescent Dye Others
    KMG-301AM TFA is the acetoxy methyl esterified form of KMG-301. KMG-301AM TFA successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg 2+-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrial membrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrial membrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg 2+ transport across the mitochondrial membrane in the early phases of a cellular model .
    KMG-301AM TFA
  • HY-14348

    5-HT Receptor Dopamine Receptor Neurological Disease
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities .
    GSK163090
  • HY-117829
    UNC9994
    1 Publications Verification

    Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin Neurological Disease
    UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
    UNC9994
  • HY-12284

    Prostaglandin Receptor Inflammation/Immunology
    NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats .
    NVP-QAV680
  • HY-14495A

    EX-1314 free base

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .
    BMS-604992 free base
  • HY-124947

    5-HT Receptor Neurological Disease
    PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI) .
    PF-4522654

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