2. Metabolic Enzyme/Protease NF-κB
  3. Phosphodiesterase (PDE) Heme Oxygenase (HO) NF-κB
  4. 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.

Neuroprotective agent 12 Chemical Structure

Neuroprotective agent 12 Chemical Structure

CAS No. : 2522599-69-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Neuroprotective agent 12 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

View All Heme Oxygenase (HO) Isoform Specific Products:

View All Isoforms
HO-1 HO-2

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

PDE4B

 

HO-1

 

In Vitro

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.

Neuroprotective agent 12 Related Antibodies

Cell Viability Assay[1]

Cell Line: HT22 cells
Concentration: 3, 10, 30, 100, and 300 μM
Incubation Time: 0.5, 24 h
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.

Western Blot Analysis[1]

Cell Line: HT22 cells, BV2 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 24 h
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.

Immunofluorescence[1]

Cell Line: HT22 cells, BV2 cells
Concentration: 3, 10 μM
Incubation Time: 24 h
Result: Significantly increased p-CREB expression.
Inhibited the nuclear translocation of NF-Κb in LPS-stimulated BV2 cells at 10 μM.
In Vivo

Neuroprotective agent 12 (Compound 5) (5-10  mg/kg, gavage administration, twice for 48 h) has significant anti-ischemic activity and neuroprotection of BBB in TBI mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 5, 10 mg/kg
Administration: Gavage administration, twice at 0 and 6 h after awaking for 48 h.
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.
Molecular Weight

380.48

Formula

C23H28N2O3
CAS No.
SMILES

COC1=C(OC2CCCC2)C=CC(/C=C/C(NC3=CC=C(N(C)C)C=C3)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Neuroprotective agent 12 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Neuroprotective agent 122522599-69-3Neuroprotective agent12Neuroprotective agent-12Phosphodiesterase (PDE)Heme Oxygenase (HO)NF-κBHeme OxygenaseNuclear factor-κBNuclear factor-kappaBNeuroprotective agentOxidative stressAnti-inflammationHT22 cellsBV2 cellsTBI mice modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Neuroprotective agent 12
Cat. No.:
HY-174339
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.