| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The binding affinity Kd value of ENDO12 (31.25 nM-3 μM) to recombinant STX7 was 2.7 µM, which was higher than that of ENDO3[1]. ENDO12 could effectively inhibit CpG-induced TLR9 activation in HEK-Blue hTLR9 cells, with an IC50 value of 1 × 10⁻⁷ M[1]. ENDO12 (10 µM; 1 h) could reduce the colocalization levels of STX7 and Munc13-4, TLR7 and LAMP1, and TLR9 and LAMP1 in RAW 264.7 mouse macrophages, thereby inhibiting endosome maturation and TLR transport[1].
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|---|---|
| ln Vivo |
ENDO12 (30 mg/kg; intraperitoneal injection; single dose; 1 hour before CpG stimulation) reduced CpG-induced systemic inflammatory response in mice and decreased plasma IL-6, IFNγ and MPO levels [1]. ENDO12 (15 mg/kg; intraperitoneal injection; single dose; 1 hour before LCMV infection) did not affect the host antiviral response to LCMV infection in mice, but only slightly reduced MIP1β and MIP2 levels [1].
|
| Cell Assay |
Immunofluorescence [1]
Cell Types: RAW 264.7 mouse macrophages Tested Concentrations: 10 µM Incubation Duration: 1 hour Experimental Results: Colocalization of STX7 with Munc13-4 was significantly reduced. Colocalization of TLR7 and TLR9 with LAMP1+ organelles was significantly reduced, indicating impaired endosome maturation and TLR transport to late lysosomes. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J mice (male and female, 6-10 weeks old)[1]
Doses: 30 mg/kg Route of Administration: Intraperitoneal injection; single dose; 1 hour before CpG stimulation Experimental Results: Compared with the control group treated with the vector, CpG-induced plasma levels of interleukin-6 (IL-6), interferon-γ (IFNγ) and myeloperoxidase (MPO) were significantly reduced. Animal/Disease Models:C57BL/6J mice (male and female, 8 weeks old)[1] Doses: 15 mg/kg Route of Administration: Intraperitoneal injection; single dose; 1 hour before LCMV infection Experimental Results: No significant changes were made to plasma IL-6, IFNα, IFNγ or MPO levels induced by LCMV infection. Only a slight decrease in plasma levels of macrophage inflammatory proteins MIP1β and MIP2 was observed, while all other cytokines and chemokines were unchanged compared to the vector control group. |
| References |
| Molecular Formula |
C15H17FN4O
|
|---|---|
| Molecular Weight |
288.32
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CCN(CC)C1=CC=C(/N=N/C2=NC=C(F)C=C2)C(O)=C1
|
| 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
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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 | 3.4684 mL | 17.3418 mL | 34.6837 mL | |
| 5 mM | 0.6937 mL | 3.4684 mL | 6.9367 mL | |
| 10 mM | 0.3468 mL | 1.7342 mL | 3.4684 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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