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| 5mg |
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L48H37 (L 48H37; L-48H37; L48H-37), a Curcumin analog with improved chemical stability, is a novel and potent myeloid differentiation 2 (MD2) inhibitor with the potential to be used for the treatment of of sepsis or lung injury. L48H37 inhibits the interaction and signaling transduction of LPS-TLR4/MD2.
| ln Vitro |
L48H37 suppresses inflammation brought on by LPS, particularly the synthesis and expression of TNF-α and IL-6 in mouse macrophages [1]. L48H37 is more effective than curcumin in lung cancer cells, reducing the viability of A549 and H460 cells with IC50 values of 2.3 µM and 5.3 µM, respectively, over a 24-hour period (0-20 µM). With an IC50 of 21 μM, it exhibits minimal cytotoxicity against normal human lung epithelial cells (BEAS-2B) [2]. L48H37 (1, 2, or 4 µM; 16 hours) enhances the expression of p53 while dose-dependently inhibiting the expression of Cdc2 and p-Cdc2. In H460 and A549 cells, it also revealed lower levels of the anti-apoptotic protein Bcl-2 and higher amounts of cleaved poly(ADP-ribosyl) polymerase (PARP) [2]. Increased DCF levels in H460 and A549 cells indicate that L48H37 (4 µM; 16 hours) rapidly and dose-dependently increases intracellular ROS levels [2].
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| ln Vivo |
L48H37 (ip; 5 mg or 10 mg/kg; once daily; 11 days) has anticancer action in mice and reduces the formation of H460 xenograft tumors [1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: A549 and H460 cells; BEAS-2B Cell Tested Concentrations: 0.625, 1.25, 2.5, 5, 7.5, 10 and 20 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of lung cancer cell growth in a concentration-dependent manner . Western Blot Analysis[2] Cell Types: A549 and H460 Cell Tested Concentrations: 0.625, 1.25, 2.5, 5, 7.5, 10 and 20 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished expression of p-Cdc2, Cdc2 and Bcl-2 in 2 lung cancers cell. |
| Animal Protocol |
Animal/Disease Models: 5weeks old athymic BALB/cA nu/nu female mice (18-22 g) [2]
Doses: 5 mg or 10 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day; 11-day Experimental Results: vs. Tumor wet weight was diminished compared to vehicle control. The levels of p-STAT3 in vivo were diminished, and the levels of p-EIF2α and ATF4 were increased. No obvious structural changes were shown in mice. |
| References |
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| Molecular Formula |
C27H33NO7
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|---|---|
| Molecular Weight |
483.56
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| Exact Mass |
483.226
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| CAS # |
343307-76-6
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| PubChem CID |
6523614
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.047
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
668
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN1C/C(=C\C2=CC(=C(C(=C2)OC)OC)OC)/C(=O)/C(=C/C3=CC(=C(C(=C3)OC)OC)OC)/C1
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| InChi Key |
IOFNKUXFKVPLPF-LQGKIZFRSA-N
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| InChi Code |
InChI=1S/C27H33NO7/c1-8-28-15-19(9-17-11-21(30-2)26(34-6)22(12-17)31-3)25(29)20(16-28)10-18-13-23(32-4)27(35-7)24(14-18)33-5/h9-14H,8,15-16H2,1-7H3/b19-9+,20-10+
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| Chemical Name |
(3E,5E)-1-ethyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one
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| Synonyms |
L48H37 L48 H37 L48-H37L 48H37L-48H 37L48H-37
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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 : ~50 mg/mL (~103.40 mM)
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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 | 2.0680 mL | 10.3400 mL | 20.6800 mL | |
| 5 mM | 0.4136 mL | 2.0680 mL | 4.1360 mL | |
| 10 mM | 0.2068 mL | 1.0340 mL | 2.0680 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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