| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
p38 MAPK ERK I-kappaBalpha IL-6 p65 NF-κB
Anti-inflammatory agent 35 targets the MAPK/ERK pathway, NF-κB, p38 MAPK, ERK, and inflammation-related signaling pathways. It blocks MAPK signaling and prevents nuclear translocation of NF-κB p65. The compound also inhibits the production of proinflammatory cytokines including TNF-α and IL-6. Its anti-inflammatory effects are mediated through the modulation of these key inflammatory pathways. |
|---|---|
| ln Vitro |
In mice, the development of pro-inflammatory cytokines (IL-6, TNF-α) by LPS (0.5 μg/mL; 24 hours) is inhibited by anti-inflammatory drug 35 (compound 5a27) (10 μM; 30 minutes). It is not cytotoxic to produce macrophages. With an IC50 of 2.40 μM and 2.23 μM, respectively, anti-inflammatory drug 35 suppresses the synthesis of TNF-α and IL-6 [1]. RAW 264.7 murine macrophages' activation caused by LPS was greatly reduced by anti-inflammatory drug 35 (10 μM; 30 min). Furthermore, it suppresses IκB levels, p-p38, and p-ERK substantially, which suggests that MAPK and NF-κB signaling are inhibited [1].
In vitro, Anti-inflammatory agent 35 exhibits dose-dependent inhibition of LPS-induced release of TNF-α and IL-6 in activated RAW 264.7 mouse macrophages, with IC50 values of 2.33 μM and 2.4 μM, respectively. It blocks MAPK signaling and nuclear translocation of NF-κB p65. The compound inhibits proinflammatory cytokine production in activated macrophages. Its anti-inflammatory activity is confirmed in multiple in vitro models. |
| ln Vivo |
Curcumin (HY-N0005) had a lower bioavailability than anti-inflammatory drug 35 (Compound 5a27) (50 mg/kg; oral; single dose, measured 0–25 minutes) [1]. By reducing inflammation in mice models, anti-inflammatory drug 35 (10 mg/kg; intraperitoneal injection; once daily for 1 week) ameliorates LPS-induced ALI [1]. Rat pharmacokinetic parameters [1]: Route Dose (mg/kg) AUC(0-t) (μg/L·h) AUC(0-∞) (μg/L·h) MRT(0-) (h) t1/2 (h) Tmax (h) CLz/F (L/h/kg) Vz/F (L/kg) Cmax po 50 231.2 325.6 7.8 12.3 6.7 3.3 5062.6 827.1 113.3 iv 5 34.3 122.4 11.3 19.9 0.2 0.1 404.4 59.5 16.4
In vivo, Anti-inflammatory agent 35 significantly attenuates LPS-induced acute lung injury (ALI). It inhibits yellow neutrophil infiltration and proinflammatory cytokine production in vivo. The compound is orally bioavailable, making it suitable for oral administration in animal studies. Its efficacy in ALI models suggests potential for treating inflammatory lung diseases. Further studies are needed to fully characterize its in vivo pharmacokinetics and therapeutic potential. |
| Enzyme Assay |
For non-cellular assays, Anti-inflammatory agent 35 is evaluated for its ability to inhibit MAPK signaling and NF-κB activation. Kinase inhibition assays are performed using purified MAPK enzymes (e.g., p38 MAPK, ERK) with appropriate substrates. NF-κB DNA binding activity is assessed using electrophoretic mobility shift assays (EMSA) or ELISA-based DNA binding assays. The compound's ability to inhibit proinflammatory cytokine production is confirmed using biochemical assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW 264.7 mouse macrophages Tested Concentrations: 10 μM Incubation Duration: 30 min; followed by incubation with 0.5 μg/mL LPS for another 30 min Experimental Results: diminished the phosphorylation of p38 and ERK. And down-regulated IκB (inhibitor of NF-κB), inhibits the transcription of TNF-α, IL-6, IL-1β, ICAM-1. In vitro cell culture experiments are performed using RAW 264.7 mouse macrophages or other immune cell lines. Cells are activated with LPS and treated with Anti-inflammatory agent 35 at concentrations ranging from 0.1 to 10 μM. Endpoints include proinflammatory cytokine levels (TNF-α, IL-6) by ELISA, NF-κB activation by reporter assays or immunofluorescence, MAPK phosphorylation by Western blot, and cell viability (MTT assay). IC50 values are calculated from dose-response curves. |
| Animal Protocol |
Animal/Disease Models: ALI mouse model (C57BL/6 mice)[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection, one time/day for 1 week; 30 min later every dose, followed by 5 mg/kg LPS, intratracheal injection Experimental Results: Dramatically normalized the wet/dry ratio of lungs. In vivo animal studies are conducted in mouse models of LPS-induced acute lung injury (ALI). Anti-inflammatory agent 35 is administered orally or intraperitoneally. Endpoints include bronchoalveolar lavage fluid (BALF) analysis (cell counts, cytokine levels), lung histology (H&E staining, inflammation score), wet/dry lung weight ratio, and survival rates. Neutrophil infiltration is assessed by myeloperoxidase (MPO) activity or immunohistochemistry. |
| ADME/Pharmacokinetics |
Anti-inflammatory agent 35 is an orally bioavailable curcumin analog. It has a molecular formula and weight as described in the literature. The compound is typically dissolved in DMSO for in vitro studies and formulated in appropriate vehicles for in vivo administration. Pharmacokinetic properties are not fully characterized, but the compound is expected to have good oral bioavailability based on its chemical properties and oral activity.
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| Toxicity/Toxicokinetics |
Anti-inflammatory agent 35 shows dose-dependent inhibition of LPS-induced TNF-α and IL-6 release with IC50 values of 2.33 μM and 2.4 μM, respectively. It blocks MAPK signaling and NF-κB p65 nuclear translocation. The compound significantly attenuates LPS-induced acute lung injury in vivo. Standard safety precautions should be followed during handling. The compound is for research use only.
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| References | |
| Additional Infomation |
Anti-inflammatory agent 35 (compound 5a27) is an orally bioavailable curcumin analog with anti-inflammatory activity. It blocks MAPK signaling and NF-κB nuclear translocation, inhibits neutrophil infiltration and proinflammatory cytokine production, and attenuates LPS-induced ALI in vivo. The compound is used in research on inflammation, acute lung injury, and inflammatory diseases. It is for research use only and is not approved for clinical use.
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| Molecular Formula |
C27H29NO8
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|---|---|
| Molecular Weight |
495.52
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| Exact Mass |
495.189
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| CAS # |
2293951-00-3
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| PubChem CID |
155549737
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
36
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| Complexity |
826
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C(=O)/C=C/C2=CC=C(OC(C)=O)C(OC)=C2)CCC/C(=C\C2=CC(OC)=C(OC)C(OC)=C2)/C1=O
|
| InChi Key |
QLGWATTXCFBRGY-ZEQSIELKSA-N
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| InChi Code |
InChI=1S/C27H29NO8/c1-17(29)36-21-10-8-18(14-22(21)32-2)9-11-25(30)28-12-6-7-20(27(28)31)13-19-15-23(33-3)26(35-5)24(16-19)34-4/h8-11,13-16H,6-7,12H2,1-5H3/b11-9+,20-13+
|
| Chemical Name |
[2-methoxy-4-[(E)-3-oxo-3-[(3E)-2-oxo-3-[(3,4,5-trimethoxyphenyl)methylidene]piperidin-1-yl]prop-1-enyl]phenyl] acetate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 16.67 mg/mL (33.64 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0181 mL | 10.0904 mL | 20.1808 mL | |
| 5 mM | 0.4036 mL | 2.0181 mL | 4.0362 mL | |
| 10 mM | 0.2018 mL | 1.0090 mL | 2.0181 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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