| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
LJ-2698 (0.1 μM, 72 h) can restore the expression of anti-inflammatory cytokines (Il4, Il10) and M2 macrophage markers (Arg1, Mrc1) in LPS-stimulated RAW 264.7 mouse macrophages [1].
|
|---|---|
| ln Vivo |
LJ-2698 (50 μg/kg; orally; 6 times a week for 5 weeks) significantly inhibited elastase-induced emphysema in FVB mice and porcine pancreas-induced emphysema by restoring lung function, reducing alveolar enlargement, inhibiting matrix metalloproteinase activity and lung cell apoptosis, and promoting M2 macrophage-mediated anti-inflammatory response, with very low observed toxicity [1]. LJ-2698 (1.5–10 mg/kg; orally; once daily for 12 weeks) improved diabetic nephropathy in db/db mice in a dose-dependent manner, with the 10 mg/kg dose showing the most stable and comprehensive renal protective effect across all assays [2].
|
| Cell Assay |
Real-time quantitative PCR [1]
Cell Types: RAW 264.7 (mouse macrophages) Tested Concentrations: 0.1 μM Incubation Duration: 48 hours (pretreatment); 24 hours (co-incubation with LPS) Experimental Results: Significantly improved the downregulation of LPS-mediated Il4 and Il10 anti-inflammatory cytokine mRNA expression. Significantly restored the downregulation of LPS-mediated Arg1 and Mrc1 M2 macrophage marker mRNA expression. |
| Animal Protocol |
Animal/Disease Models:FVB mice (8 weeks old) [1]
Doses: 50 μg/kg Route of Administration: Oral; 6 times a week for 5 weeks Experimental Results: Lung compliance and tissue elasticity were restored to near the level of the control group. PPE-induced alveolar expansion was significantly inhibited and the PPE-induced mean linear intercept (MLI) increase was reduced. PPE-mediated increase in matrix metalloproteinase gelatinase activity in lung tissue was inhibited. The number of TUNEL-positive apoptotic cells in lung tissue was significantly reduced compared with mice treated with PPE alone. The downregulation of anti-inflammatory cytokines (IL-4, IL-10) and M2 macrophage markers (Arg1, Mrc1/CD206) mRNA expression in lung tissue induced by PPE was restored. The number of CD206-positive M2 macrophages per field of view in lung tissue was increased. Compared with the control group or the group that used PPE only, no significant changes in body weight were observed, indicating extremely low toxicity. Animal/Disease Models:C57BLKS/J-db/db (male, 8 weeks old) [2] Doses: 1.5 mg/kg; 5 mg/kg; 10 mg/kg Route of Administration: Oral; Daily; 12 weeks Experimental Results: All three doses significantly reduced elevated glomerular volume and mesangial area, with no significant difference between doses. 5 mg/kg and 10 mg/kg doses significantly reduced elevated urinary albumin excretion; 1.5 mg/kg dose did not produce a significant reduction. 10 mg/kg dose significantly inhibited the decrease in renin mRNA levels and the increase in NGAL mRNA levels. 10 mg/kg dose significantly inhibited the increase in TGF-β mRNA levels; no significant reduction was observed at 1.5 and 5 mg/kg doses. At doses of 5 and 10 mg/kg, the increase in collagen IV and fibronectin mRNA levels was significantly reduced. At doses of 5 and 10 mg/kg, the increase in MCP-1 mRNA levels was significantly reduced; at a dose of 10 mg/kg, the increase in ICAM-1 mRNA levels was significantly inhibited, while doses of 1.5 and 5 mg/kg had no such effect. At doses of 5 and 10 mg/kg, the increase in urinary LPO levels was significantly reduced. |
| References |
|
| Molecular Formula |
C16H15CL2N5O2S
|
|---|---|
| Molecular Weight |
412.29
|
| CAS # |
945457-84-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
N(CC1=CC(Cl)=CC=C1)C2=C3C(N(C=N3)[C@H]4[C@H](O)[C@H](O)CS4)=NC(Cl)=N2
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 2.4255 mL | 12.1274 mL | 24.2548 mL | |
| 5 mM | 0.4851 mL | 2.4255 mL | 4.8510 mL | |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4255 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
