SJ-300
SJ-300 is a potent and selective, orally active and brain-penetrat DKK3-LRP1 interaction inhibitor. SJ-300 restores Aβ clearance in AD models. SJ 300 binds to mLRPIV with a Kd of 7.9 μM, inhibits the DKK3 mLRPIV complex with an IC50 of 3.2 μM, and does not disrupt the binding of Aβ to LRP1. SJ 300 rescues cognitive function and ameliorates neuropathology (Aβ plaque reduction ≈ 73.3 %) in vivo. SJ 300 can be employed for research in Alzheimer’s disease.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1210357-06-4
- 分子式: C20H27FN4
- 分子量:342.45
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
SJ-300 (0-5 μM) exerts a substantial reduction in the DKK3-mLRPIV interaction in SH-SY5Y cells[1].
SJ-300 (1 μM, 2 h) restores Aβ internalization in AD-NSC cells[1].
SJ-300 (10 μM) has no direct impact on the canonical Wnt/β-catenin signaling pathway in SH-SY5Y cell. [1].
SJ-300 (50 μM in 2 μL0-60 min) has superior metabolic stability in mouse and human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AD-NSC cell
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Concentration:1 μM
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Incubation Time:2 h
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Result:Restored Aβ internalization in cells treated with DKK3 but in treated with DKK1.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-24 | AUC0-inf | Vz-F_obs | MRT | F | ClF_obs |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | i.g. | 11.2 h | 1 h | 178 ng/mL | 1721 ng·h/mL | 2280 ng·h/mL | 72973 mL/h/kg | 7.7965 h | 71.30 % | / |
| Mice | 2 mg/kg | i.v. | 11.2 h | 0.079 h | 74.2 ng/mL | 483 ng·h/mL | 538 ng·h/mL | 52931 mL/kg | 7.2043 h | / | 3732 mL/h/kg |
SJ-300 (i.g., 10 mg/kg, once) shows a brain-penetration capability with brain/plasma (B/P) ratio = 5732 %[1].
SJ-300 (i.g., 5 mg/kg, once daily for 8 weeks) improves cognitive functions in the 5×FAD transgenic mouse (6 months) model of AD, and these improvements associate with reductions in Aβ pathology.[1].
SJ-300 (i.g., 5 mg/kg, once daily for 8 weeks) attenuates cognitive deficits and AD pathologies through enhancing Aβ clearance in 6-month-old 5×FAD mice.[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5×FAD transgenic mouse model of AD (16 weeks)[1]
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Dosage:5 mg/kg
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Administration:i.g., once daily for 8 weeks
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Result:Reduced escape latencies during the 5-day acquisition phase.
Increased time spent in the target quadrant, and number of platform crossings during the probe trials.
Enhanced spatial working memory in the Y-maze test.
Reduced the number of Aβ plaques of various diameters in both brain regions.
Decreased the total number of Aβ plaques by approximately 73.3%.
Decreased the clustering of astrocytes by 64.1 % and microglia around the plaques.
Reduced both soluble and insoluble Aβ levels.
Did not affect APP cleavage or Aβ production.
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Animal Model:5×FAD transgenic mouse model of AD (6 months)[1]
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Dosage:5 mg/kg
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Administration:i.g., once daily for 8 weeks
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Result:Did not alter LRP1 expression but reduced colocalized Aβ on brain vascular basement membranes and endothelium.
Reduced the levels of both Aβ40 and Aβ42 in the plasma and liver of treated mice.
Did not alter the circulating concentrations of soluble LRP1.
Inhibited the association between soluble LRP1 (sLRP1) and DKK3.
化学情報
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CAS 番号 1210357-06-4
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分子量 342.45
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分子式 C20H27FN4
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SMILES
FC1=CC=C(N2N=C(C)C(CNC3CCN(C4CC4)CC3)=C2C)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SJ-300 関連分類
HY-179459 関連分類
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