| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
MAPK signaling pathway, with downstream suppression of JNK and p38 phosphorylation. The compound also inhibits AChE (IC50 23.84 µM) and reduces NO, IL-1β, IL-6, and TNF-α release in LPS-stimulated BV-2 microglial cells, indicating combined MAPK-pathway and anti-neuroinflammatory mechanisms.
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| ln Vitro |
The release of NO, IL-1β, IL-6, and TNF-α in BV-2 cells is inhibited by MAPK-IN-1 (Compound 2), with IC50 values of 0.49 ± 0.17, 1.34 ± 0.21, 9.17 ± 0.17, and 8.17 ± 0.23 μM, respectively [1]. The phosphorylation of JNK, ERK, and p38 in the LPS-induced MAPK signaling pathway is downregulated by MAPK-IN-1 [1]. In BV-2 cells, MAPK-IN-1 suppresses the production of iNOS, COX-2, and TLR4 that is stimulated by LPS [1].
MAPK-IN-1 inhibits AChE with an IC50 of 23.84 µM. In BV-2 microglial cells, it suppresses LPS-induced NO production and reduces pro-inflammatory cytokine release, supporting anti-neuroinflammatory activity at micromolar concentrations. The compound is described as having neuroprotective activity in the context of Alzheimer's disease research. |
| ln Vivo |
Publicly available in vivo efficacy data for this specific compound are limited. The compound is described as having anti-neuroinflammatory and neuroprotective activity and is proposed for Alzheimer's disease research, but compound-specific behavioral, biochemical, and pharmacokinetic data in animal models require confirmation from primary literature.
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| Enzyme Assay |
AChE inhibition is measured using Ellman's assay, in which acetylthiocholine is hydrolyzed by AChE to thiocholine, which reacts with DTNB to produce a yellow chromophore. Serial dilutions of compound are pre-incubated with AChE, and absorbance at 412 nm is monitored. IC50 values are calculated from the inhibition of the initial reaction rate.
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| Cell Assay |
BV-2 microglial cells are seeded in 96-well plates and stimulated with LPS in the presence or absence of serial dilutions of MAPK-IN-1. After 24 hours, culture supernatants are collected for NO (Griess assay) and cytokine quantification by ELISA. Cell viability is measured in parallel. For MAPK pathway analysis, cell lysates are immunoblotted for phospho-JNK, phospho-p38, and phospho-ERK.
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| Animal Protocol |
For neuroinflammation models, compound is administered systemically to mice, and neuroinflammation is induced by intracerebroventricular or intraperitoneal LPS injection. Brain tissue is collected for cytokine measurement, microglial activation markers (Iba1), and MAPK phosphorylation. Behavioral tests such as the Morris water maze or novel object recognition may be used to assess cognitive outcomes in Alzheimer's disease models.
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| References |
| Molecular Formula |
C19H18O4
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|---|---|
| Molecular Weight |
310.34
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| Exact Mass |
310.12
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| CAS # |
2470587-69-8
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| PubChem CID |
164516862
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| Appearance |
Orange to red solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
23
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| Complexity |
642
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O1C[C@H](C)C2C(=O)C(=O)C3=C(C1=2)C=CC1=C3CCC(=O)C1(C)C
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| InChi Key |
ABVRZQXICIZPLM-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C19H18O4/c1-9-8-23-18-11-4-6-12-10(5-7-13(20)19(12,2)3)15(11)17(22)16(21)14(9)18/h4,6,9H,5,7-8H2,1-3H3/t9-/m0/s1
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| Chemical Name |
(1R)-1,6,6-trimethyl-1,2,8,9-tetrahydronaphtho[1,2-g][1]benzofuran-7,10,11-trione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~322.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2223 mL | 16.1114 mL | 32.2227 mL | |
| 5 mM | 0.6445 mL | 3.2223 mL | 6.4445 mL | |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2223 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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