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BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). It reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells, improves scopolamine-induced cognitive impairment, alleviates LPS-induced spatial learning deficits, and exhibits anti-neuroinflammatory effects in mice, making it applicable for Alzheimer's disease (AD) research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). It reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells, improves scopolamine-induced cognitive impairment, alleviates LPS-induced spatial learning deficits, and exhibits anti-neuroinflammatory effects in mice, making it applicable for Alzheimer's disease (AD) research. |
| Targets&IC50 | p38α MAPK:191 nM |
| In vitro | BChE/p38-α MAPK-IN-1 (Compound 95) exhibits inhibitory activity against hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). At concentrations of 1-5 μM over 18 hours, it reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in phytohemagglutinin (PHA)-stimulated human peripheral blood mononuclear cells (PBMCs) and slightly increases the anti-inflammatory cytokine IL-12. |
| In vivo | BChE/p38-α MAPK-IN-1 (Compound 95), when administered intraperitoneally at 5-10 mg/kg 60 minutes prior to testing, improves scopolamine-induced cognitive impairment in adult male albino Swiss (CD-1) mice. Additionally, BChE/p38-α MAPK-IN-1, at a dosage of 10 mg/kg via intraperitoneal injection once daily for 10 days, alleviates spatial learning deficits induced by LPS and exhibits anti-neuroinflammatory effects in adult male C57BL/6J mice. |
| Molecular Weight | 454.57 |
| Formula | C26H32F2N4O |
| Cas No. | 3077831-11-6 |
| Smiles | O=C(NCCN(C)C)C1=CC2=C(C=NN2CC3CCCCC3)C=C1CC4=CC=C(F)C=C4F |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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