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allosteric effects

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51

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3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120837
    PZ-II-029

    		GABA Receptor Neurological Disease
    PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .
    PZ-II-029
  • HY-10915
    LUF6096

    		Adenosine Receptor Cardiovascular Disease
    LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury .
    LUF6096
  • HY-142618
    TNF-α-IN-6

    		TNF Receptor Inflammation/Immunology
    TNF-α-IN-6 (compound 12) is an orally effective allosteric inhibitor of TNFα (KD = 6.8 nM). TNF-α-IN-6 has anti-inflammatory effects .
    TNF-α-IN-6
  • HY-139644
    MIPS521

    		Adenosine Receptor Neurological Disease
    MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine .
    MIPS521
  • HY-107111
    GSK1034702

    		Cholinesterase (ChE) Neurological Disease
    GSK1034702 is a M1 mAChR allosteric agonist. GSK1034702 shows procognitive effects in rodents. GSK1034702 modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction .
    GSK1034702
  • HY-163180
    AKT-IN-22

    		Akt Cancer
    AKT-IN-22 (compound 0R4) is a potent AKT allosteric inhibitor with anticancer effects .
    AKT-IN-22
  • HY-117979
    Alphadolone

    Alfadolone

    		 GABA Receptor Neurological Disease
    Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia .
    Alphadolone
  • HY-128783
    VU0090157

    		mAChR Neurological Disease
    VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
    VU0090157
  • HY-107111A
    GSK1034702 hydrochloride

    		Cholinesterase (ChE) Neurological Disease
    GSK1034702 hydrochloride is a M1 mAChR allosteric agonist. GSK1034702 hydrochloride shows procognitive effects in rodents. GSK1034702 hydrochloride modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction .
    GSK1034702 hydrochloride
  • HY-15786
    SGE-201

    		iGluR Neurological Disease
    SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.
    SGE-201
  • HY-137067
    IMT1B
    5 Publications Verification

    LDC203974

    		 DNA/RNA Synthesis Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .
    IMT1B
  • HY-151949
    TrkA-IN-4

    		Trk Receptor Neurological Disease
    TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects .
    TrkA-IN-4
  • HY-145684
    EP2 receptor antagonist-1

    		Prostaglandin Receptor Inflammation/Immunology
    EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .
    EP2 receptor antagonist-1
  • HY-107663
    MIF-1

    Pro-Leu-Gly-NH2; Melanostatin

    		 Dopamine Receptor Neurological Disease
    MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
    MIF-1
  • HY-119256
    COR627

    		GABA Receptor Neurological Disease
    COR627 is a GABA receptor positive allosteric modulator with the ability to enhance GABA activity. COR627 exhibits effects on GABA and baclofen stimulation in rat cortical membranes and can increase its affinity for GABA(B) receptors. In vivo experiments have shown that COR627 can enhance the sedative/hypnotic effects of baclofen at pretreatment ineffective doses .
    COR627
  • HY-119082A
    VU0029767

    		mAChR Others
    VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
    VU0029767
  • HY-110180
    VU0409106

    		mGluR Neurological Disease
    VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
    VU0409106
  • HY-100979
    W-84 dibromide

    HDMPPA

    		 mAChR Others
    W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
    W-84 dibromide
  • HY-107663A
    MIF-1 TFA

    Pro-Leu-Gly-NH2 TFA; Melanostatin TFA

    		 Dopamine Receptor Neurological Disease
    MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
    MIF-1 TFA
  • HY-119082
    (E/Z)-VU0029767

    		mAChR Others
    (E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
    (E/Z)-VU0029767
  • HY-B0520AS1
    Benztropine-d3 mesylate

    		Dopamine Receptor Histamine Receptor mAChR Cancer
    Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
    Benztropine-d3 mesylate
  • HY-12509
    PEPA

    		iGluR Neurological Disease
    PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects .
    PEPA
  • HY-152207
    LWG-301

    		Glutaminase Apoptosis Cancer
    LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .
    LWG-301
  • HY-B0520AS
    Benztropine-13C,d3 mesylate

    		Isotope-Labeled Compounds Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
    Benztropine-13C,d3 mesylate
  • HY-169432
    TET-13

    		GABA Receptor Neurological Disease
    TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively) .
    TET-13
  • HY-149602
    Glutaminase C-IN-2

    		Glutaminase Reactive Oxygen Species Cancer
    Glutaminase C-IN-2 (compound 11) is glutaminase C (GAC) allosteric inhibitor with an IC50 of 10.64 nM. Glutaminase C-IN-2 regulates the cellular metabolite, thereby increasing reactive oxygen species (ROS) by blocking glutamine metabolism. Glutaminase C-IN-2 has anticancer effects .
    Glutaminase C-IN-2
  • HY-B0520A
    Benztropine mesylate
    5 Publications Verification

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    		 Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine mesylate
  • HY-B0520
    Benztropine

    Benzatropine; Benzotropine

    		 Dopamine Receptor mAChR Histamine Receptor Cancer
    Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine
  • HY-N0240
    Herbacetin
    4 Publications Verification

    		 Ornithine decarboxylase (ODC) Cancer
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .
    Herbacetin
  • HY-100939
    4-Chlorophenylguanidine hydrochloride

    		Sodium Channel Neurological Disease
    4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
    4-Chlorophenylguanidine hydrochloride
  • HY-154848
    UCL-TRO-1938
    1 Publications Verification

    		 PI3K Akt Cardiovascular Disease Neurological Disease Cancer
    UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush .
    UCL-TRO-1938
  • HY-114169S
    WRG-28-d5

    		Isotope-Labeled Compounds Cancer
    WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic
    WRG-28-d5
  • 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-121600
    GAT229

    		Cannabinoid Receptor
    GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure .
    GAT229
  • HY-114169
    WRG-28

    		Discoidin Domain Receptor Inflammation/Immunology Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
    WRG-28
  • HY-B0520AR
    Benztropine (mesylate) (Standard)

    Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)

    		 Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine (mesylate) (Standard)
  • HY-108204
    AZD 3043

    THRX 918661

    		 GABA Receptor Others
    AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
    AZD 3043
  • HY-115860
    TAS-4

    		iGluR Neurological Disease
    TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
    TAS-4
  • HY-49444
    EN450

    		NF-κB Molecular Glues E1/E2/E3 Enzyme Cancer
    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
    EN450
  • HY-120327
    KY-226
    2 Publications Verification

    		 Phosphatase Neurological Disease Metabolic Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
    KY-226
  • HY-161296
    TH6342

    		Bacterial HIV Infection
    TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
    TH6342
  • HY-N0240R
    Herbacetin (Standard)

    		Others Cancer
    Herbacetin (Standard) is the analytical standard of Herbacetin. This product is intended for research and analytical applications. Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .
    Herbacetin (Standard)
  • HY-117902
    SRI-31142

    		Dopamine Transporter Neurological Disease
    SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .
    SRI-31142
  • HY-103565
    AMN082
    1 Publications Verification

    		 mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
    AMN082
  • HY-13509
    CCG-50014
    2 Publications Verification

    		 RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
    CCG-50014
  • HY-120355A
    AP14145 hydrochloride

    		Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
    AP14145 hydrochloride
  • HY-171177
    P5SA-2

    		Phosphatase Neurological Disease Cancer
    P5SA-2 is a selective allosteric activator of PPP5C. P5SA-2 exerts its effects by modulating the phosphatase domain of PPP5C and can increase PPP5C activity by 3.2-fold at 100 μM with an apparent affinity constant of 7.8 μM. P5SA-2 can be used in cancer and Alzheimer's disease research .
    P5SA-2
  • HY-103565A
    AMN082 free base
    1 Publications Verification

    		 mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
    AMN082 free base
  • HY-156025
    HCAR2 agonist 1

    		Hydroxycarboxylic Acid Receptor (HCAR) Inflammation/Immunology
    HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
    HCAR2 agonist 1
  • HY-117734
    PYD-106

    		iGluR Neurological Disease
    PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors .
    PYD-106

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