| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KB-0118 (1–10 μM, 12 h) downregulated pro-inflammatory cytokines (e.g., TNF, MIF, and CSF2) in PMA/roximycin (6)-treated Jurkat cells [1]. KB-0118 (1–10 μM, 12 h) downregulated pro-inflammatory cytokines (e.g., IL-1β, IL-6, IL-23a, and Cxcl11) in LPS-treated RAW 264.7 cells [1]. KB-0118 (5 μM, 5 days) inhibited the proliferation of anti-CD3 and anti-CD28 activated mouse CD4+ T cells, manifested by a decrease in cell division, proliferation, expansion, and replication indices [1]. KB-0118 (5 μM, 5 days) reduced the proportion of Th17 cells (RORγt+ IL-17A+), indicating that it inhibited Th17 cell differentiation [1]. KB-0118 (5 μM, 5 days) increased the proportion of Th2 cells (GATA-3+ IL-4+), indicating that it can promote Th2 polarization [1]. KB-0118 (0.01-1 μM, 24 hours) improved the survival rate of Caco-2 cells treated with DSS (5%, 48 hours) [1].
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|---|---|
| ln Vivo |
KB-0118 (200 mg/kg, dissolved in drinking water, for 7 consecutive days) alleviated colitis symptoms in a mouse model of DSS (3% dissolved in drinking water) induced by DSS [1]. KB-0118 (50 mg/kg, orally, once daily for 6 weeks) alleviated T-cell-mediated colitis by reducing the IL-17a-driven inflammatory response in a mouse model of chronic T-cell-mediated colitis [1]. KB-0118 (50–250 mg/kg, orally, for 14 consecutive days) showed good tolerability in both male and female C57BL/6 mice [1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: Jurkat cells Tested Concentrations: 1 μM, 5 μM, 10 μM Incubation Duration: Pretreatment for 6 hours, followed by co-incubation with PMA/roxithromycin for 6 hours Experimental Results: The expression of pro-inflammatory cytokines, particularly TNF, MIF, CSF2, and TGFB1, was downregulated, and these downregulations were statistically significant at concentrations of 5 μM and 10 μM. The expression of IL-3, IL-4, and IL-26 was upregulated. |
| Animal Protocol |
Animal/Disease Models:A male C57BL/6 mouse colitis model induced by DSS (3% concentration in drinking water) was used [1].
Doses: 200 mg/kg Route of Administration: Added to drinking water for 7 consecutive days Experimental Results: Compared with the DSS-only group, this study showed a significant protective effect on colon length, maintained colon integrity, and reduced inflammation. Compared with the DSS-only group, this study reduced epithelial damage and immune cell infiltration. Compared with the DSS-only group, this study slightly reduced body weight and disease activity index (DAI), but the difference was not statistically significant. Animal/Disease Models:A chronic colitis model induced by adoptive transfer of CD45RBhigh T cells into RAG1 KO mice [1]. Doses: 50 mg/kg Route of Administration: Oral gavage (po), once daily for 6 weeks Experimental Results: Compared with the vector control group, the mice showed reduced body weight and increased colon length. Reduced colonic epithelial damage and immune cell infiltration, demonstrating superior efficacy compared to MS402. IL-17a levels were decreased in the DSS-treated colon. Downregulation of key genes for T cell activation and cytotoxicity (e.g., Cd3e, Lck, and Stat4) and integrin genes (e.g., Itgam and Itgal) was observed (batch RNA sequencing). Reduced expression of genes regulated by immune-related transcription factors (e.g., IRF8, FOXO1, and RUNX1) was observed (batch RNA sequencing). |
| References |
| Molecular Formula |
C17H11NO5
|
|---|---|
| Molecular Weight |
309.27
|
| CAS # |
2648377-08-4
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C1C(O)=C(C2=CC3=C(C=CN3)C=C2)OC4=C1C(O)=CC(O)=C4
|
| Synonyms |
BBC0115
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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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.2334 mL | 16.1671 mL | 32.3342 mL | |
| 5 mM | 0.6467 mL | 3.2334 mL | 6.4668 mL | |
| 10 mM | 0.3233 mL | 1.6167 mL | 3.2334 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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