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α5

" in MedChemExpress (MCE) Product Catalog:

71

Inhibitors & Agonists

3

Biochemical Assay Reagents

8

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1

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4

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15

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2

Isotope-Labeled Compounds

9

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1

Oligonucleotides

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 .
    α5IA
  • 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.
    α5β1 integrin agonist-1
  • HY-103510

    GABA Receptor Neurological Disease
    TB-21007 is a selective and brain penetrant α5 subunit-containing GABAA receptor inverse agonist with Kis of 1.6 nM, 20 nM, 16 nM, and 20 nM for α5, α1, α2 and α3 subtypes, respectively. TB-21007 enhances cognition in rats .
    TB-21007
  • HY-112788

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
    ONO-8590580
  • HY-120874

    PF-06372865; CVL-865

    GABA Receptor Neurological Disease
    Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat 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. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
    Darigabat
  • 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-14426
    L-655708
    3 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-170771

    GABA Receptor Neurological Disease
    α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders .
    α5-GABAA receptor modulator 1
  • HY-I0563

    α-(5-Bromo-2-fluorophenyl)benzo[b]thiophene-2-methanol

    Drug Intermediate Others
    Benzo[b]thiophen-2-yl(5-bromo-2-fluorophenyl)methanol (α-(5-Bromo-2-fluorophenyl)benzo[b]thiophene-2-methanol) is a drug intermediate for synthesis of various active compounds.
    Benzo[b]thiophen-2-yl(5-bromo-2-fluorophenyl)methanol
  • HY-173251S

    GABA Receptor Neurological Disease
    ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .
    ENX-101
  • HY-123426

    GABA Receptor
    JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors .
    JY-XHe-053
  • HY-100370
    MRK-016
    1 Publications Verification

    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 GABAA α5β3γ2, 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-120051
    Afizagabar
    2 Publications Verification

    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-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-N2160

    GABA Receptor Neurological Disease
    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 .
    L-838417-d9
  • 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-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-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-109009
    Padsevonil
    1 Publications Verification

    UCB-0942

    GABA Receptor Neurological Disease
    Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
    Padsevonil
  • 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-100369AR

    Reference Standards GABA Receptor Neurological Disease
    DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • 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-109009A

    (S)-UCB-0942

    GABA Receptor Neurological Disease
    (S)-Padsevonil is the S-enantiomer of Padsevonil (HY-109009).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
    (S)-Padsevonil
  • 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-111052R

    GABA Receptor Cytochrome P450 Neurological Disease Inflammation/Immunology
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. 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 (Standard)
  • HY-10233R

    Lu 02-030 hydrochloride (Standard); THIP hydrochloride (Standard)

    Reference Standards GABA Receptor Neurological Disease
    Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-132806

    RG-7816; RO-7017773

    GABA Receptor Neurological Disease
    Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .
    Alogabat
  • HY-137393

    Drug Metabolite Metabolic Disease
    3α,5α-Tetrahydronorethisterone is the major urinary metabolites of Norethisterone (HY-B0554) .
    3α,5α-Tetrahydronorethisterone
  • 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 .
    Alpha-5-Methyluridine
  • HY-101274A

    G protein-coupled Bile Acid Receptor 1 FXR Cardiovascular Disease
    (3α, 5β, 6β, 7α)-BAR501 (BAR504-6b) is a compound having cholane scaffolds of formula. (3α, 5β, 6β, 7α)-BAR501 can be used for the research of FXR and TGR5/GPBAR1 mediated diseases .
    (3α,5β,6β,7α)-BAR501
  • 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 (3α,5α)-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-150124

    Integrin Apoptosis Cancer
    K34c is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c can be used in glioblastoma research .
    K34c
  • HY-150124A

    Integrin Apoptosis Cancer
    K34c hydrochloride is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c hydrochloride reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c hydrochloride can be used in glioblastoma research .
    K34c hydrochloride
  • 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-129953A

    5-trans PGF2α

    Endogenous Metabolite Cardiovascular Disease
    5-trans Prostaglandin F2α is an endogenous metabolite present in Blood that can be used for the research of Myocardial Infarction .
    5-trans Prostaglandin F2α
  • HY-W722556

    3α,5α-Androstanol

    GABA Receptor Constitutive Androstane Receptor Metabolic Disease
    5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms .
    5α-Androstan-3α-ol
  • HY-164768

    Integrin Cancer
    LT25 (compound 17) is a agonist of α5β1 integrin with EC50 value of 9.9 nM .
    LT25
  • HY-P99333
    Volociximab
    1 Publications Verification

    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-13535
    ATN-161
    5+ Cited Publications

    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-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-115854

    GABA Receptor Neurological Disease
    Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions .
    Ro 15-1310
  • HY-P10704

    Integrin Cancer
    C16Y is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .
    C16Y

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