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Results for "

α5

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

3

Biochemical Assay Reagents

6

Peptides

1

Inhibitory Antibodies

2

Natural
Products

13

Recombinant Proteins

1

Isotope-Labeled Compounds

5

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-116622

    L-822179

    GABA Receptor Neurological Disease
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .
    <em>α5</em>IA
  • HY-139702

    Integrin Cancer
    α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
    <em>α5</em>β1 integrin agonist-1
  • HY-112788

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
    ONO-8590580
  • HY-16716
    Basmisanil
    1 Publications Verification

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
    Basmisanil
  • HY-120874

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
    PF-06372865
  • HY-14426
    L-655708
    1 Publications Verification

    GABA Receptor Neurological Disease
    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
    L-655708
  • HY-132806

    RG-7816; RO-7017773

    GABA Receptor Neurological Disease
    Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .
    Alogabat
  • HY-100370

    GABA Receptor Cancer
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAAα5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
    MRK-016
  • HY-147657

    GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
    GABAA receptor modulator-2
  • HY-114871

    GABA Receptor Neurological Disease
    SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities .
    SL651498
  • HY-120051

    S44819; Egis-13529

    GABA Receptor Neurological Disease
    Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
    Afizagabar
  • HY-N2160

    6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons .
    6'''-Feruloylspinosin
  • 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[1].
    L-838417-d9
  • HY-100369A

    GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5  receptors, respectively .
    DMCM hydrochloride
  • HY-123840

    GABA Receptor Neurological Disease
    MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .
    MRK-623
  • HY-107669

    nAChR Neurological Disease
    nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1 hydrochloride
  • HY-107489

    GABA Receptor Neurological Disease
    RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
    RO 4938581
  • HY-14571
    E7820
    4 Publications Verification

    ER68203-00

    Molecular Glues Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity .
    E7820
  • HY-151129

    nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    nAChR-IN-1
  • HY-111052

    GABA Receptor Cytochrome P450 Neurological Disease Inflammation/Immunology
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
    AZD7325
  • HY-W009009

    GABA Receptor Neurological Disease
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
    L-838417
  • HY-10233
    Gaboxadol hydrochloride
    1 Publications Verification

    Lu 02-030 hydrochloride; THIP hydrochloride

    GABA Receptor Neurological Disease
    Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent .
    Gaboxadol hydrochloride
  • HY-153584

    GABA Receptor Neurological Disease
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
    MRK-898
  • HY-154540

    Nucleoside Antimetabolite/Analog Cancer
    Alpha-5-Methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
    <em>Alpha-5</em>-Methyluridine
  • HY-W127431

    5α-Cholanic acid-3α-ol-6-one 3-acetate methyl ester

    Biochemical Assay Reagents Others
    Methyl (3α,5α)-3-(acetyloxy)-6-oxocholan-24-oate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Methyl (3<em>α,5</em>α)-3-(acetyloxy)-6-oxocholan-24-oate
  • HY-111413

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM .
    c(phg-isoDGR-(NMe)k)
  • HY-111413A

    Integrin Cancer
    c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM .
    c(phg-isoDGR-(NMe)k) TFA
  • HY-P5038

    c(GRGDSP)

    Integrin Cancer
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)
  • HY-P99333

    M200; Eos 200-4

    Integrin Cardiovascular Disease Cancer
    Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs) .
    Volociximab
  • HY-13535A
    ATN-161 trifluoroacetate salt
    5+ Cited Publications

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161 trifluoroacetate salt
  • HY-13535

    Integrin Cancer
    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161
  • HY-150124

    Integrin Cancer
    K34c is a potent and selective α5β1 integrin antagonist. K34c can be used for glioblastoma research .
    K34c
  • HY-103510

    GABA Receptor Neurological Disease
    TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats .
    TB-21007
  • HY-15682
    TTNPB
    3 Publications Verification

    Ro 13-7410; Arotinoid acid; AGN191183

    RAR/RXR Autophagy Apoptosis Cancer
    TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
    TTNPB
  • HY-P1189

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1 .
    Echistatin
  • HY-P1189A

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1 .
    Echistatin TFA
  • HY-P1740
    RGD peptide (GRGDNP)
    3 Publications Verification

    Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
    RGD peptide (GRGDNP)
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)
    3 Publications Verification

    Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
    RGD peptide (GRGDNP) (TFA)
  • HY-15102
    MK-0429
    3 Publications Verification

    L-000845704

    Integrin Inflammation/Immunology Cancer
    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
    MK-0429
  • HY-103512

    GABA Receptor Neurological Disease
    TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
    TP003
  • HY-12706

    R 5188

    Adrenergic Receptor 5-HT Receptor Neurological Disease Inflammation/Immunology
    Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect .
    Spiroxatrine
  • HY-156521

    Integrin Others
    αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of integrins ανβ1 and α5β1 with IC50s of 0.9 nM,and 33 nM,respectively. αvβ1 integrin-IN-2 also inhibits other integrins with ,,IC50s of 380 nM (ανβ3),280 nM (ανβ5),230 nM (ανβ6),87 nM (ανβ8),respectively,in SPRA assay .
    αvβ1 integrin-IN-2
  • HY-16141
    Cilengitide
    Maximum Cited Publications
    38 Publications Verification

    EMD 121974

    Integrin Autophagy Apoptosis STAT PD-1/PD-L1 Cancer
    Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers .
    Cilengitide
  • HY-103521

    GABA Receptor Neurological Disease
    Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo .
    Anxiolytic/nonsedative agent-1
  • HY-14565

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
    Pozanicline
  • HY-129453

    Integrin Inflammation/Immunology
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
    BOP sodium
  • HY-121638A
    (5Z,2E)-CU-3
    1 Publications Verification

    Apoptosis DGK Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
    (<em>5</em>Z,2E)-CU-3
  • HY-125777A

    nAChR Neurological Disease
    α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach .
    α-Conotoxin Vc1.1 TFA
  • HY-121638

    Apoptosis DGK Inflammation/Immunology Cancer
    CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
    CU-3

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