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Results for "

subtype selectivity

" in MedChemExpress (MCE) Product Catalog:

198

Inhibitors & Agonists

3

Screening Libraries

9

Peptides

8

Natural
Products

7

Isotope-Labeled Compounds

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-103229

    iGluR Neurological Disease
    Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
    Cl-HIBO
  • HY-103066

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2, α2β4, α4β2, α4β4, (α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1-0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
    Br-PBTC
  • HY-133012

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
    GFB-8438
  • HY-B0374A

    BDF5895 hydrochloride

    Imidazoline Receptor Neurological Disease
    Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
    Moxonidine hydrochloride
  • HY-101308A
    MRS2179 tetrasodium hydrate
    2 Publications Verification

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
    MRS2179 tetrasodium hydrate
  • HY-142723

    Potassium Channel Neurological Disease
    KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype .
    KCa2 channel modulator 1
  • HY-142735

    Potassium Channel Neurological Disease
    KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively
    KCa2 channel modulator 2
  • HY-115764

    nAChR Neurological Disease
    nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM) .
    nAChR agonist 2
  • HY-150692

    Estrogen Receptor/ERR Cancer
    Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
    Estrogen receptor α antagonist 1
  • HY-101308

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
    MRS2179 tetrasodium
  • HY-142868

    Prostaglandin Receptor Neurological Disease
    ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist.
    ONO-8713
  • HY-123414

    PF-05196233

    Sodium Channel Neurological Disease
    GX-936 (PF-05196233), a potent and Nav1.7-subtype selective inhibitor, binds to the activated state of voltage-sensor domain IV (VSD4) .
    GX-936
  • HY-P1219

    β-TRTX-Cj1α

    Sodium Channel Neurological Disease
    Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
    Jingzhaotoxin-III
  • HY-125382

    Somatostatin Receptor Metabolic Disease
    L-797591 is a selective somatostatin receptor subtype 1 (SSTR1) agonist .
    L-797591
  • HY-B0374

    BDF5895

    Imidazoline Receptor Cardiovascular Disease Neurological Disease
    Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
    Moxonidine
  • HY-12811

    Sodium Channel Neurological Disease
    PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
    PF-04856264
  • HY-142908

    Endogenous Metabolite Cancer
    Maximiscin, a fungal metabolite, induces DNA damage and shows selective cytotoxic activity against a subtype of triple-negative breast cancer.
    Maximiscin
  • HY-14319B

    nAChR Neurological Disease
    Sazetidine A dihydrochloride is a potent ligand for the α4β2 nAChR, with high binding affinity and selectivity for this subtype. Sazetidine A dihydrochloride exhibits favorable pharmacological properties and may contribute to research targeting nicotinic receptor-related diseases. Sazetidine A dihydrochloride has been mentioned in studies investigating the binding affinity of various analogs, highlighting its importance in understanding the nAChR ligand subtype selectivity .
    Sazetidine A dihydrochloride
  • HY-15831

    Isotope-Labeled Compounds GABA Receptor Neurological Disease
    L-838417-d9 is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes .
    L-838417-d9
  • HY-163317

    Somatostatin Receptor Cancer
    MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC can be used for the research of cancer .
    MMC(TMZ)-TOC
  • HY-12439
    ML380
    1 Publications Verification

    mAChR Neurological Disease
    ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
    ML380
  • HY-162117

    mGluR Neurological Disease
    LBG30300 is a subtype-selective mGlu2 receptor agonist EC50 0.6 nM. LBG30300 is blood-brain barrier permeable .
    LBG30300
  • HY-163317A

    Somatostatin Receptor Cancer
    MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer .
    MMC(TMZ)-TOC TFA
  • HY-157889

    HDAC Cancer
    ZINC000028464438 is a selective HDAC11 inhibitor with an IC50 of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes .
    ZINC000028464438
  • HY-101869

    MRK-409

    GABA Receptor Neurological Disease
    MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
    MK-0343
  • HY-14319A

    nAChR Neurological Disease
    Sazetidine A hydrochloride is a potent ligand for the α4β2 nicotinic acetylcholine receptor, exhibiting high binding affinities and selectivity towards this subtype. Sazetidine A hydrochloride demonstrates promising pharmacological properties that could potentially contribute to the development of therapies targeting nicotinic receptor-related conditions. Sazetidine A hydrochloride has been implicated in studies examining the binding affinities of various analogs, highlighting its significance in understanding subtype selectivity among nAChR ligands.
    Sazetidine A hydrochloride
  • HY-164964

    LPL Receptor Neurological Disease
    TRV045 is a selective Sphingosine-1-phosphate subtype 1 receptor agonist with no effect on lymphocyte transport. TRV045 has antiepileptic activity .
    TRV045
  • HY-101640

    GABA Receptor Neurological Disease
    TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
    TPA 023
  • HY-101254R

    N-0774 (Standard)

    Reference Standards Melatonin Receptor Neurological Disease
    Luzindole (Standard) is the analytical standard of Luzindole. This product is intended for research and analytical applications. Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
    Luzindole (Standard)
  • HY-101254
    Luzindole
    Maximum Cited Publications
    12 Publications Verification

    N-0774

    Melatonin Receptor Neurological Disease
    Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
    Luzindole
  • HY-19630

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ML289
  • HY-108498

    Somatostatin Receptor Endocrinology
    L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions
    L-817818
  • HY-W037331

    Bis(4-fluorophenyl)methanol

    mAChR Others
    4,4-Difluorobenzhydrol is a precursor of a mAChR antagonist, and its derivative 4,4-Difluorobenzhydrol Carbamate can selectively target the M1 subtype .
    4,4-Difluorobenzhydrol
  • HY-107713

    iGluR Neurological Disease
    PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D containing receptors .
    PPDA
  • HY-111271A

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
    L 888607 Racemate
  • HY-117196

    PPAR Metabolic Disease Inflammation/Immunology
    GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity .
    GW 9578
  • HY-147664

    Carbonic Anhydrase Cancer
    These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
    hCAXII-IN-1
  • HY-150727

    Sirtuin Cancer
    SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively .
    SIRT5 inhibitor 4
  • HY-15393

    mGluR Neurological Disease
    VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .
    VU 0357121
  • HY-N0584A

    6-Hydroxyhyoscyamine hydrobromide

    mAChR Inflammation/Immunology Cancer
    Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties .
    Anisodamine hydrobromide
  • HY-167824

    Endogenous Metabolite Neurological Disease
    SSR180711 is a potent and subtype-selective α7 agonist with activity in Alzheimer's disease and schizophrenia research. SSR180711 can be used to study subtypes of intracerebral hemorrhage associated with cerebral small vessel disease. SSR180711 shows potential in electrophysiological and behavioral studies to evaluate its effects on cognitive function. SSR180711 also has potential for studying cerebrovascular lesions and their effects .
    SSR180711
  • HY-169345

    mGluR Neurological Disease
    VU6043653 is a potent, selective and cross the blood-brain barrier metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 value of 325 nM for h mGlu5 .
    VU6043653
  • HY-128770
    LY3154207
    1 Publications Verification

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
    LY3154207
  • HY-15072

    YM 872

    iGluR Metabolic Disease
    Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
    Zonampanel
  • HY-14342
    MK-5046
    2 Publications Verification

    Bombesin Receptor Metabolic Disease
    MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
    MK-5046
  • 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-116046

    Melatonin Receptor Others
    GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice .
    GR 196429
  • HY-14312

    nAChR Neurological Disease
    A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile .
    A85380
  • HY-103183

    2-Phenylaminoadenosine

    Adenosine Receptor Endogenous Metabolite Inflammation/Immunology
    CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively .
    CV1808
  • HY-114191B

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM) .
    SSTR5 antagonist 2 hydrochloride

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