2227316-74-5
2227316-74-5 structure
- Name: GSK-3β inhibitor 13
- Chemical Name: GSK-3β inhibitor 13
- CAS Number: 2227316-74-5
- Molecular Formula: C23H22N6O2
- Molecular Weight: 414.46
- Catalog: Signaling Pathways Epigenetics PKC
- Create Date: 2023-04-21 13:23:31
- Modify Date: 2024-01-11 22:30:33
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GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease[1].
| Name | GSK-3β inhibitor 13 |
|---|
| Description | GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease[1]. |
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| Related Catalog | |
| Target |
GSK-3β:0.73 nM (IC50) GSK-3α:0.35 nM (IC50) PKCθ:0.36 μM (IC50) PIM1:0.38 μM (IC50) AAK1:0.20 μM (IC50) |
| In Vivo | GSK-3β inhibitor 13 在血浆中的暴露量为 3.8 μM，在脑中的暴露量为 1.3 μM，导致脑-血浆 (B/P) 比率为 0.34[1]。 GSK-3β inhibitor 13 (30 mg/kg；口服；单剂量) 在 LaFerla 3xTg-C57BL6 小鼠中降低 52% 的 pTau396 水平[1]。 在小鼠中的药代动力学分析[1] Route Dose (mg/kg) CL (mL/mL/kg) Vss (L/kg) MRT (h) t1/2 (h) i.v. 2 3.8 1.1 4.8 5.2 Route Dose (mg/kg) AUCtot (μM·h) Cmax (μM) F (%) p.o. 10 68.3 7.8 64 |
| References |
| Molecular Formula | C23H22N6O2 |
|---|---|
| Molecular Weight | 414.46 |