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.
For research use only. We do not sell to patients.
- CAS No.: 2522599-69-3
- Formula: C23H28N2O3
- Molecular Weight:380.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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 No. 2522599-69-3
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Molecular Weight 380.48
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Neuroprotective agent 12 Related Classifications
HY-174339 Related Classifications
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