Search Result
Results for "
allosteric effects
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-120837
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GABA Receptor
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Neurological Disease
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PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .
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- HY-10915
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Adenosine Receptor
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Cardiovascular Disease
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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 .
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- HY-142618
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- HY-139644
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Adenosine Receptor
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Neurological Disease
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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 .
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- HY-137067
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IMT1B
Maximum Cited Publications
6 Publications Verification
LDC203974
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DNA/RNA Synthesis
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Cancer
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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 .
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- HY-151949
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Trk Receptor
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Neurological Disease
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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 .
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- HY-163180
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Akt
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Cancer
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AKT-IN-22 (compound 0R4) is a potent AKT allosteric inhibitor with anticancer effects .
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- HY-117979
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Alfadolone
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GABA Receptor
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Neurological Disease
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Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia .
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- HY-128783
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mAChR
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Neurological Disease
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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 .
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- HY-15786
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iGluR
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Neurological Disease
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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.
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- HY-145684
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Prostaglandin Receptor
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Inflammation/Immunology
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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 .
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-
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- HY-107663
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Pro-Leu-Gly-NH2; Melanostatin
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Dopamine Receptor
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Neurological Disease
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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) .
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- HY-119256
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GABA Receptor
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Neurological Disease
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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 .
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-
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- HY-119082A
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mAChR
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Others
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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.
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- HY-110180
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mGluR
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Neurological Disease
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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) .
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- HY-117132
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mGluR
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Neurological Disease
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YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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- HY-100979
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HDMPPA
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mAChR
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Others
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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 .
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-
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- HY-103556
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mGluR
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Neurological Disease
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YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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- HY-107663A
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Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
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Dopamine Receptor
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Neurological Disease
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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) .
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- HY-119082
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mAChR
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Others
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(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.
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- HY-12509
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iGluR
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Neurological Disease
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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 .
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- HY-152207
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Glutaminase
Apoptosis
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Cancer
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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 .
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- HY-169432
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GABA Receptor
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Neurological Disease
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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) .
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- HY-149602
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Glutaminase
Reactive Oxygen Species (ROS)
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Cancer
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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 .
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- HY-B0520A
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Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
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Dopamine Receptor
mAChR
Histamine Receptor
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Neurological Disease
Cancer
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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 .
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- HY-B0520
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Benzatropine; Benzotropine
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Dopamine Receptor
mAChR
Histamine Receptor
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Cancer
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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 .
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- HY-N0240
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Ornithine decarboxylase (ODC)
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Cancer
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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 .
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- HY-154848
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PI3K
Akt
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Cardiovascular Disease
Neurological Disease
Cancer
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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 .
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- HY-114169S
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Isotope-Labeled Compounds
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Cancer
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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
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- HY-121600
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Cannabinoid Receptor
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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 .
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- HY-109009
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UCB-0942
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GABA Receptor
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Neurological Disease
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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 .
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- HY-B0520AS1
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Dopamine Receptor
Histamine Receptor
mAChR
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Cancer
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Benztropine-d3 (mesylate) is the 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 .
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- HY-114169
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WRG-28
1 Publications Verification
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Discoidin Domain Receptor
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Inflammation/Immunology
Cancer
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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 .
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- HY-B0520AR
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Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)
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Reference Standards
Dopamine Receptor
mAChR
Histamine Receptor
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Neurological Disease
Cancer
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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 .
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- HY-108204
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THRX 918661
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GABA Receptor
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Others
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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.
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- HY-115860
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iGluR
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Neurological Disease
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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 .
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- HY-49444
-
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NF-κB
Molecular Glues
E1/E2/E3 Enzyme
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Cancer
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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 .
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- HY-120327
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KY-226
2 Publications Verification
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Phosphatase
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Neurological Disease
Metabolic Disease
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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 .
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- HY-101165
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iGluR
GABA Receptor
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Neurological Disease
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Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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- HY-100939
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Sodium Channel
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Neurological Disease
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4-Chlorophenylguanidine hydrochloride is an urokinase-type plasminogen activator inhibitor. 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 .
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- HY-B0520AS
-
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Isotope-Labeled Compounds
Dopamine Receptor
mAChR
Histamine Receptor
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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 .
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- HY-161296
-
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Bacterial
HIV
|
Infection
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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 .
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- HY-N0240R
-
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Reference Standards
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 .
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- HY-117902
-
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Dopamine Transporter
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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 .
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- HY-103565
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AMN082
1 Publications Verification
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mGluR
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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 .
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- HY-109009A
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(S)-UCB-0942
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GABA Receptor
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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 .
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- HY-13509
-
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RGS Protein
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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 .
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- HY-107111
-
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mAChR
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Neurological Disease
|
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-107111A
-
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Cholinesterase (ChE)
mAChR
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Neurological Disease
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GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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- HY-101165R
-
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Reference Standards
iGluR
GABA Receptor
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Neurological Disease
|
Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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- HY-120355A
-
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Potassium Channel
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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) .
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- HY-171177
-
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Phosphatase
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Neurological Disease
Cancer
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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 .
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- HY-103565A
-
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mGluR
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Neurological Disease
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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 .
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- HY-103565R
-
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Reference Standards
mGluR
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Neurological Disease
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AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. 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 .
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- HY-156025
-
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Hydroxycarboxylic Acid Receptor (HCAR)
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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 .
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- HY-13509R
-
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RGS Protein
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Inflammation/Immunology
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CCG-50014 (Standard) is the analytical standard of CCG-50014. This product is intended for research and analytical applications. 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 .
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- HY-117734
-
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iGluR
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Neurological Disease
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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 .
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- HY-103565AR
-
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Reference Standards
mGluR
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Neurological Disease
|
AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. 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 .
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- HY-173397
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β-glucuronidase
Bacterial
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Metabolic Disease
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β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric β-glucuronidase inhibitor. β-Glucuronidase-IN-3 has potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) (IC50: 12.9 nM). β-Glucuronidase-IN-3 exerts its inhibitory effect by reversibly covalently modifying the cysteine residues (Cys28, Cys443, and Cys197) of EcGUS. β-Glucuronidase-IN-3 can be used in the study of intestinal microbiota-related diseases, especially to alleviate the toxic side effects of Irinotecan (HY-16562) and nonsteroidal anti-inflammatory drugs (NSAIDs) .
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- HY-16639
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GPR35
Neurotensin Receptor
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Neurological Disease
Endocrinology
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ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
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- HY-115857
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GABA Receptor
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Neurological Disease
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SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
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HY-L170
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216 compounds
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An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 216 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
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Product Name |
Target |
Research Area |
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- HY-107663A
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Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
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Dopamine Receptor
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Neurological Disease
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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) .
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- HY-107663
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Pro-Leu-Gly-NH2; Melanostatin
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Dopamine Receptor
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Neurological Disease
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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) .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-114169S
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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
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- HY-B0520AS1
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Benztropine-d3 (mesylate) is the 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 .
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- HY-B0520AS
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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 .
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