(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.
For research use only. We do not sell to patients.
- CAS No.: 1235733-73-9
- Formula: C20H27N3OS
- Molecular Weight:357.51
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Storage:
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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Biological Activity
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Chemical Information
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- Purity & Documentation
- References
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Biological Activity
Description
In Vitro
(Rac)-AF710B is a highly potent and selective ligand for M1 mAChR and σ1R, with no significant off-target activity against 83 other GPCRs, ion channels, and transporters[1].
(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. Further protocols information, click here.
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].
(Rac)-AF710B (10 μg/kg/day; i.p.; for 2 months) alleviates cognitive impairment in the 3xTg-AD mouse model and attenuates AD-like pathological changes, including Aβ accumulation, tau pathology, and neuroinflammation[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 No. 1235733-73-9
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Molecular Weight 357.51
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Formula C20H27N3OS
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SMILES
O=C(CCC1=CNC2=C1C=CC=C2)N3CC4(CCN(CC4)C)SC3C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-AF710B Related Classifications
HY-116586A Related Classifications
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