MW073
MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].
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- CAS No.: 3048608-87-0
- Formule: C22H27N5
- Masse moléculaire:361.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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5-HT2B Receptor 70 nM (IC50) |
MW073 (0.1-10 μM) demonstrates that its biochemical mechanism of action for both h5-HT2BR (Kd = 86 nM, EC50Gprotein = 1.1 μM, EC50β-Arrestin1 = 2.4 μM) and m5-HT2BR (Kd = 125 nM, EC50Gprotein = 6.7 μM, EC50β-Arrestin1 = 0.6 μM) is the dose-dependent inhibition of both serotonin-induced activation/β-arrestin-1 recruitment and basal constitutive activity in transfected HEK293A cells, suggesting inverse agonism[1].
MW073 exhibits only 5-HT2BR antagonist activity when subjected to large-scale cellular screening of 165 diverse G Protein-Coupled Receptors (GPCRs) for agonist and antagonist activity using a panel of stably transfected CHO cell lines[1].
MW073 exhibits no activity against kinases, key enzymes, or transporters, and its lack of CYP450 substrate status predicts low drug-interaction potential[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MW073 (0-5 mg/kg, p.o., q.d. for 30-45 days starting at the age of day 60-70) dose-dependently prevents and ameliorates memory deficits in APP/PS1 mice[1].
MW073 (5 mg/kg, p.o., q.d. for ~150-250 days) restores synaptic and memory function in hTau/Mapt-KO mice, proving effective in both preventive and therapeutic intervention paradigms during chronic treatment[1].
MW073 (5 mg/kg, i.p., q.d. for 3 weeks) reduces aggressive behavior without inducing sedation or hypoactivity in Tg2576 mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (3-4 months old) infused with 200 nM Aβ- or 500 nM tau-oligomers or vehicle (intrahippocampal, 20 min prior to test)[1]
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Dosage:5 mg/kg
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Administration:i.p., 30 min prior to test
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Result:Attenuates both Aβ- and tau-oligomer-induced synaptic dysfunction.
Rescued long-term potentiation (LTP) deficit in hippocampal slices treated with Aβ or tau oligomers (perfused at 1.9 µM).Reduced errors in the 2-day radial arm water maze (RAWM) induced by Aβ or tau oligomers.
Attenuated both Aβ- and tau-oligomer–induced reduction in freezing in the contextual fear conditioning (FC).
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Animal Model:hTau/Mapt-KO mice (7 months old)[1]
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Dosage:5 mg/kg
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Administration:p.o., q.d. for ~250 days (prior to significant pathology)
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Result:Prevented the impairment of LTP.
Re-established the normal number of errors in the RAWM (~180 days).
Protected against the impairment of associative memory in contextual FC (~240 days).
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Animal Model:APP/PS1 transgenic mice (3-4 months old)[1]
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Dosage:0-5 mg/kg
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Administration:p.o., q.d. for 30-45 days starting at the age of day 60-70
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Result:Dose-dependently reduced the number of errors in the radial arm water maze (RAWM).
Ameliorated the contextual FC defect in a dose-dependent manner.
ED50 for RAWM improvement was 1.886 mg/kg.
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Animal Model:hTau/Mapt-KO mice (11 months old)[1]
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Dosage:0-5 mg/kg
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Administration:p.o, q.d. for ~150 days (after pathology onset)
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Result:Restored the capability of undergoing LTP.
Protected against the impairment of spatial memory in the RAWM (~45 days).
Protected against the impairment of associative memory in contextual FC (~140 days).
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Animal Model:Male Tg2576 mice[2]
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Dosage:5 mg/kg
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Administration:i.p., q.d. for 3 weeks
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Result:Significantly reduced aggressive behavior compared to the vehicle control group in the resident-intruder test.
Decreased the duration of the first attack.
Decreased the number of attacks and the total attack time.
Revealed no significant differences in the time spent in the center versus the periphery of the arena, number of entries into the center, and total distance traveled.
Did not alter locomotor function, anxiety-like behavior, or exploratory activity.
Chemical Information
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CAS No. 3048608-87-0
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Masse moléculaire 361.48
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Formule C22H27N5
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SMILES
CN1CCN(CC1)CCNC2=NN=C(C=C2C)C3=CC=C4C=CC=CC4=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MW073 Related Classifications
HY-178323 Related Classifications
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