(Rac)-AF710B
(Rac)-AF710B is the racemate of AF710B (HY-116586). (Rac)-AF710B is an orally active and blood-brain barrier-penetrant σ1 receptor (σ1R) agonist and M1 muscarinic acetylcholine receptor (M1 mAChR) allosteric agonist. (Rac)-AF710B can be used for research on Alzheimer's disease.
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- CAS. Nr.: 1235733-73-9
- Formel: C20H27N3OS
- Molecular Weight:357.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
In Vitro
(Rac)-AF710B (0.1-10 nM; 3 h) significantly enhances the binding affinity of Carbachol (Carbamoylcholine chloride) (HY-B1208) to M1 mAChR and the downstream phosphorylation of p-ERK1/2 and p-CREB in PC12M1 cells at nanomolar concentrations[1].
(Rac)-AF710B (30 nM) almost completely rescues mushroom spine loss in hippocampal neurons of PS1-KI and APP-KI Alzheimer's disease model mice, an effect that depends on M1 mAChR activation and σ1R expression[1].
(Rac)-AF710B reduces tau phosphorylation and increases the inactive form of GSK3β in PC12M1 cells through an M1 mAChR-dependent mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
(Rac)-AF710B (10 μg/kg; p.o.) exerts its anti-amnesic effects at least partially through σ1R activation in the Trihexyphenidyl model, as the σ1R antagonist NE-100 significantly blocks its cognitive-enhancing effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (Male, 225-250 g, 3 months old)[1]
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Dosage:1-100 μg/kg
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Administration:p.o.; single administration
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Result:Significantly prolonged retention latency at 1, 3, 10, and 30 μg/kg compared to DDW-treatedTrihexyphenidyl rats.
Did not affect retention latency at 100 μg/kg.
Significantly differed between 10 μg/kg and 100 μg/kg doses.
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Animal Model:Wistar rats (Male, 225-250 g, 3 months old)[1]
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Dosage:10 μg/kg
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Administration:p.o.; single administration
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Result:Significantly prolonged retention latency to 361.7 s compared to DDW-treated Trihexyphenidyl rats.
Co-administration with NE-100 (1 mg/kg, p.o.) significantly blocked the antiamnesic effect, reducing retention latency to 185.4 s.
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Animal Model:3xTg-AD mice (Female, harboring PS1M146V, APPKM670/671ML, and tauP301L mutations, 10-12 months old)[1]
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Dosage:10 μg/kg/day
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Administration:i.p.; for 2 months
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Result:Improved cognitive function during training and probe sessions of the Morris water maze.
Significantly reduced levels of Aβ40 and Aβ42 in detergent soluble and insoluble fractions.
Significantly decreased thioflavin S-positive plaques.
Significantly diminished expression of BACE1 and levels of C99.
Reduced p-tau (AT100, AT8, AT180, AT270, PHF-1 epitopes).
Significantly increased phosphorylation of GSK3β at Ser9 and diminished p25 fragment levels.
Resulted in significantly fewer reactive astrocytes and activated microglia.
Chemical Information
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CAS. Nr. 1235733-73-9
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Molecular Weight 357.51
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Formel C20H27N3OS
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SMILES
O=C(CCC1=CNC2=C1C=CC=C2)N3CC4(CCN(CC4)C)SC3C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(Rac)-AF710B Related Classifications
HY-116586A Related Classifications
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