| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
p38 MAPK ERK I-kappaBalpha IL-6 p65 NF-κB
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|---|---|
| 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].
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| 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
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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. |
| 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. |
| References |
[1]. Qian J, et al. Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). Eur J Med Chem. 2019 Apr 1;167:414-425.
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| Molecular Formula |
C27H29NO8
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|---|---|
| Molecular Weight |
495.52
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| CAS # |
2293951-00-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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
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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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