BLINK15
BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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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。
- 分子式: C24H19BrN2O6
- 分子量:511.32
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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
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CDK9/Cyclin T 74.63 nM (IC50) |
CDK1/Cly Y 35.84 nM (IC50) |
CDK2/ClyA2 44.12 nM (IC50) |
CDK5/p35 29.34 nM (IC50) |
Cdk5/p25 12.08 nM (IC50) |
BLINK15 (50 nM-100 nM, 24 h) lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM)[1].
BLINK15 (50 nM-100 nM, 24 h) shows declined CDK5 activity in N2A cell lines overexpressing CDK5/p35 and CDK5/p25[1].
BLINK15 (25-500 μM, 24 h) maintains cell viability above 50% at all doses in HEK293T, HepG2, and N2A cell lines[1].
BLINK15 (100-500 μM, 7 h) shows the ability to traverse the BBB and access the central nervous system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High-fat diet (HFD)-fed (3-4 weeks), four-week-old male C57BL/6J mice (n=40)[1]
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Dosage:20 mg/kg/day, 40 mg/kg/day
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Administration:Intraperitoneal injection (i.p.), 20 days, 3 months after HFD-fed for 3-4 weeks
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Result:Demonstrated rescued symptoms caused by T2D including gaining of body weight, glucose tolerance test (GTT) and insulin tolerance test (ITT) level.
Alleviated cognitive impairment including rescued muscle strength and prevent anxiety, showing mitigated adverse effects of HFD level.
Rescued memory and spatial learning impairments in T2D mouse models with 40 mg/kg/day dosage but no effect with 20 mg/kg/day.
Significantly reduced CDK5 activity even in the presence of p25.
化学情報
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分子量 511.32
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分子式 C24H19BrN2O6
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SMILES
O[C@](C1=C(N2CC3=CC=CC=C3)C=CC(Br)=C1)(CC(C4=CC([N+]([O-])=O)=C(OC)C=C4)=O)C2=O
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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)
BLINK15 関連分類
HY-173348 関連分類
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