SCR1693
SCR1693 is a selective, reversible, orally active and noncompetitive inhibitor of AChE (IC50 = 0.68 μM) as well as a calcium channel blocker. SCR1693 reduces tau phosphorylation levels, and inhibits the generation and release of Aβ. SCR1693 restores insulin signaling and improves cognitive deficits. SCR1693 can be used for the study of Alzheimer's disease, especially which complicated with type 2 diabetes mellitus.
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- CAS No.: 1442559-20-7
- Formule: C24H28ClN3O2
- Masse moléculaire:425.95
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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
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
AChE |
In Vitro
SCR1693 (0.4-5 μM, 24 h) reduces total and phosphorylated tau levels in HEK293/tau cells[1].
SCR1693 (0.8-20 μM, 6 h) induces tau dephosphorylation and increases total tau levels in HEK293/tau cells with short-term treatment[1].
SCR1693 (0.4-4 μM, 24 h) inhibits Aβ generation and release in N2a/APP cells[1].
SCR-1693 (3.3-30 μM, 6 h) downregulates tau phosphorylation mainly by regulating its phosphatases in Neuro-2a-tau cells[2].
SCR-1693 (10 μM , 6 h) activates PKA/Akt, inhibits GSK-3β, and enhances PP2A/PP1 activity in Neuro-2a-tau cells[2].
SCR-1693 (10 μM, 6 h) reduces insulin resistance by regulating PP1/PP2A in Neuro-2a-tau cells[2].
SCR-1693 (0.004-2.5 μM, 48 h) inhibits Aβ25-35 (HY-P0128)-induced SH-SY5Y cell death[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293/tau cells
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Concentration:0.4, 2, 5 μM
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Incubation Time:24 h
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Result:Increased tau dephosphorylation level at Ser198/199/202 sites (Tau 1 epitope) concentration dependently.
Reduced total tau level significantly at 5 μM.
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Cell Line:HEK293/tau cells
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Concentration:0.8, 4, 20 μM
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Incubation Time:6 h
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Result:Induced tau dephosphorylation at Ser198/199/202 (Tau-1) sites and increased total tau level (4 μM and 20 μM).
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Cell Line:Neuro-2a-tau cells
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Concentration:3.3, 10, 30 μM
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Incubation Time:6 h
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Result:Decreased tau phosphorylation levels at the sites of Ser199/202, Ser202/T205, T212/Ser214, Thr231, Ser262 and Ser356, rather than Ser422,and increased tau dephosphorylation level.
Activated PKA and Akt, and inhibited GSK-3β activation.
Decreased the negatively regulated phosphorylation of PP2AC and PP1 at the site of Tyr307 and Thr320, respectively.
Enhanced PP2A and PP1 activity.
Enlarged insulin signaling, especially p-IRS-1 Tyr632 and p-Akt Ser473.
In Vivo
SCR1693 (3-30 mg/kg, p.o. single dose) dose-dependently causes the inhibition of brain homogenate AChE activity in wistar rats[3].
SCR1693 (0.1-1 mg/kg, p.o., once daily, 12 days) improves spatial memory in Aβ25-35-treated mice [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:STZ (3 mg/kg) was administered intracerebroventricularly twice in male wistar rats (220-250 g)[2]
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Dosage:1, 2, 4 mg/kg
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Administration:i.g., once daily for 20 days
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Result:Shortened STZ-injection induced lengthening of escape latency during the training period.
Showed a significant improvement of behavioral performance in the probe trails test.
Restored the levels of GPAF and PSD-95.
Decreased STZ-induced tau hyperphosphorylation in hippocampus of rats.
Decreased deactivated phosphorylation of PP1 and PP2A in a dose-dependent manner.
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Animal Model:A single intracerebroventricular (icv) injection of aggregated Aβ25-35 in mice[3]
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Dosage:0.1, 0.3, 1 mg/kg
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Administration:p.o. once daily for 12 days
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Result:Improved Aβ25-35-impaired learning and both long-term and short-term memory and its effects were stronger than Donepezil (HY-14566) and Memantine (HY-B0591).
Decreased AChE activity.
Prevented Aβ25-35-induced loss of hippocampal pyramidal cells.
Protected hippocampal synaptic transmission and LTP.
Regulated hippocampal protein phosphorylation in Aβ25–35-treated mice.
Chemical Information
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CAS No. 1442559-20-7
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Masse moléculaire 425.95
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Formule C24H28ClN3O2
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SMILES
O=C(C1=C(C)N=C2NC3=C(CC(C)(CC3)C)C(N)=C2C1C4=C(Cl)C=CC=C4)OCC
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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
[1]. Wang XL, et al. A novel tacrine-dihydropyridine hybrid (-)SCR1693 induces tau dephosphorylation and inhibits Aβ generation in cells. Eur J Pharmacol. 2015 May 5;754:134-9. [Content Brief]
[2]. Bi A, et al. SCR-1693 inhibits tau phosphorylation and improves insulin resistance associated cognitive deficits. Neuropharmacology. 2020 May 15;168:108027. [Content Brief]
[3]. Zhang Z, et al. A novel acetylcholinesterase inhibitor and calcium channel blocker SCR-1693 improves Aβ25-35-impaired mouse cognitive function. Psychopharmacology (Berl). 2016 Feb;233(4):599-613. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SCR1693 Related Classifications
HY-165341 Related Classifications
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