Neuroprotective agent 12
Neuroprotective agent 12 is an orally active and BBB-penetrable neuroprotective agent. Neuroprotective agent 12 has potent neuroprotective effects with robust anti-oxidation and anti-inflammation. Neuroprotective agent 12 significantly inhibits glutamate- and acrolein-induced cell death, reduces PDE4B expression but increases the HO-1, p-CREB and BDNF levels. Neuroprotective agent 12 exhibits potent neuroprotection in traumatic brain injury (TBI) mice model, promising for TBI and other central nervous system diseases.
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- CAS. Nr.: 2522599-69-3
- Formel: C23H28N2O3
- Molecular Weight:380.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PDE4B |
HO-1 |
Neuroprotective agent 12 (Compound 5) (24 h) reverses the cell death induced by glutamate or acrolein in HT22 cells[1].
Neuroprotective agent 12 (3-300 μM, 0.5-24 h) has no cytotoxicity under 100 μM, significantly reduces the glutamate- or acrolein-induced cytotoxicity in HT22 cells[1].
Neuroprotective agent 12 interactions with the PDE4D activity pocket without effects on the activities of PDE4B2 and PDE4D7[1].
Neuroprotective agent 12 (1-10 μM, 24 h) significantly increases the protein levels of p-CREB, BDNF and HO-1, and modulates the PDE/CREB pathway by directly decreasing PDE4B protein in HT22 cells [1].
Neuroprotective agent 12 (1-10 μM, 1 μg/mL LPS, 24 h) inhibits LPS (HY-D1056)-induced neuroinflammation through modulating the NF-κB pathway and dose-dependently reduces NO released in LPS-stimulated BV2 cells[1].
Neuroprotective agent 12 has good intestinal absorption and BBB penetration, inhibits CYP2C19, CYP2C9, and CYP2D6 but not CYP1A2 and Pgp substrate with low toxicity (LD50: 300-5000 mg/kg) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT22 cells
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Concentration:3, 10, 30, 100, and 300 μM
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Incubation Time:0.5, 24 h
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Result:Had great neuroprotective activity on glutamate- and acrolein-induced death on HT22 cells.
Protected 75.8% and 100.5% cell viability by glutamate induced at 3 and 10 μM, respectively.
Protected 72.8% and 96.4% cell viability by acrolein induced at 3 and 10 μM, respectively.
Had no cytotoxicity under 100 μM, and Significantly reduced the glutamate- or acrolein-induced cytotoxicity.
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Cell Line:HT22 cells, BV2 cells
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Concentration:1, 3, 10, 30 μM
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Incubation Time:24 h
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Result:Significantly increased the protein levels of p-CREB, BDNF and HO-1.
Decreased the protein level of PDE4B.
Notably decreased the nuclear protein level of NF-Κb in LPS-stimulated BV2 cells at 10 μM.
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Cell Line:HT22 cells, BV2 cells
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Concentration:3, 10 μM
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Incubation Time:24 h
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Result:Significantly increased p-CREB expression.
Inhibited the nuclear translocation of NF-Κb in LPS-stimulated BV2 cells at 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Kun Ming mice (8 weeks old) were shot twice with rubber bullet at right hemisphere (3 mm lateral and 1 mm posterior to the bregma) to establish TBI mice model.[1].
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Dosage:5, 10 mg/kg
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Administration:Gavage administration, twice at 0 and 6 h after awaking for 48 h.
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Result:Reduced the bleeding area and repaired the damaged BBB in TBI mice model.
Significantly decreased the hemorrhagic area in a dose-dependent manner in TBI mice model.
Effectively attenuated the Evans Blue leakage induced by TBI.
Reduced the protein levels of MMP2 and MMP9 in TBI mice model.
Chemical Information
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CAS. Nr. 2522599-69-3
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Molecular Weight 380.48
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Formel C23H28N2O3
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SMILES
COC1=C(OC2CCCC2)C=CC(/C=C/C(NC3=CC=C(N(C)C)C=C3)=O)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Neuroprotective agent 12 Related Classifications
HY-174339 Related Classifications
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