| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
UF7996 (compound 10) (10 μM) was able to displace the binding of [3H]CCR2-RA-[R] in U2OS-CCR2 cells, with a pKi of 6.9 nM and an inhibition rate of <50%[1]. LUF7996 (0.1-31.6 μM, treated for 2 hours) did not show significant degradation ability in HEK293-LgBiT cells at concentrations below 1 μM; however, it showed significant degradation ability at concentrations above 1 μM, rapidly and in a concentration-dependent manner degrading CCR2 DC50 = 5.6 μM without a “hook effect”; Dmax = 85% at 31.6 μM and 79% at 10 μM[1]. LUF7996 binds to CCR2 with an IC50 of 7.858 μM, exhibiting a strong CRBN recruitment effect with an IC50 of 143 μM [1]. CCR2 degradation mediated by LUF7996 (10 μM, 12 or 24 h of treatment) was rescued upon co-treatment with a CRBN inhibitor (competitive binding site) or a CRBN degrader [1]. LUF7996 (10 μM, 3 h of treatment) resulted in a significant increase in CCR2 ubiquitination, indicating that it degrades CCR2 at least partially through a CRBN and ubiquitin-dependent mechanism [1]. LUF7996 (10 μM, 0-25 h) did not block CCR2 degradation when co-treated with the proteasome inhibitor Bortezomib or MG-132 (10 μM) or the neddylation inhibitor MLN-4924 (250 nM), but instead enhanced degradation after 16 h, indicating that its mechanism of action is independent of the proteasome and nydration [1]. The CCR2 degradation effect of LUF7996 (10 μM, 0-25 h) can be blocked by inhibiting the lysosomal pathway, as evidenced by the complete recovery of CCR2 levels when co-treated with bafilomycin-A1 (Baf-A1) and the observed reduction in degradation when co-treated with Chloroquine [1]. LUF7996 (10 μM, 24 h) resulted in a significant reduction in [3H]CCR2-RA-[R] binding in THP-1 cells, indicating a decrease in CCR2 levels [1]. LUF7996 (10 μM) showed a potent 84% inhibition of CCL2-induced monocyte migration in THP-1 cells [1].
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|---|---|
| References |
| Molecular Formula |
C39H34CL2F3N5O8S
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|---|---|
| Molecular Weight |
860.68
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| CAS # |
3104736-80-0
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
ClC1=CC=C(OC2=CC=C(C(NCCCCCCNC3=CC=CC(C(N4C5CCC(NC5=O)=O)=O)=C3C4=O)=O)C=C2)C(NS(C6=CC=C(Cl)C(C(F)(F)F)=C6)(=O)=O)=C1
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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)
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| 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 | 1.1619 mL | 5.8094 mL | 11.6187 mL | |
| 5 mM | 0.2324 mL | 1.1619 mL | 2.3237 mL | |
| 10 mM | 0.1162 mL | 0.5809 mL | 1.1619 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
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