| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
MIF (Macrophage Migration Inhibitory Factor).
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|---|---|
| ln Vitro |
RDR 03785 is a covalent MIF inhibitor with an IC50 of 0.36 microM. It irreversibly binds to MIF, inhibiting its tautomerase activity and blocking downstream pro-inflammatory signaling. At this potency, the compound effectively reduces MIF-dependent cellular responses, including cytokine production and cell migration.
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| ln Vivo |
No in vivo activity data for RDR 03785 is publicly available. For MIF inhibitors in general, in vivo models include LPS-induced septic shock, collagen-induced arthritis, or tumor xenograft models. MIF knockout or inhibition reduces TNF-alpha, IL-1beta, and IL-6 levels, improves survival, and reduces tumor growth. RDR 03785 is expected to show similar anti-inflammatory effects.
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| Enzyme Assay |
Not available. A generic MIF tautomerase activity assay is used. Recombinant human MIF (50-100 nM) is incubated with varying concentrations of RDR 03785 (0.1 nM-10 microM) in assay buffer (50 mM sodium phosphate buffer pH 7.2, 0.5 mM EDTA, 0.1 mM DTT, 0.1% BSA) for 15-30 min at 25degC. Substrate (L-dopachrome methyl ester, 0.5 mM) is added, and the tautomerase reaction is monitored by absorbance decrease at 475 nm for 2-5 min (spectrophotometer). IC50 is calculated from the rate of reaction inhibition. Covalent inhibition can be confirmed by pre-incubation without substrate.
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| Cell Assay |
Human THP-1 monocytes or RAW264.7 macrophages are seeded in 6-well plates (1×10⁶/well) in RPMI-1640 with 10% FBS. Cells are treated with RDR 03785 (0.1-10 microM) for 1 h, then stimulated with LPS (100 ng/mL) for 6-24 h. Supernatants are collected for TNF-alpha, IL-6, and IL-1beta ELISA. Cell lysates are analyzed by Western blot for MIF protein levels and phosphorylation of ERK, p38, and NF-kappaB. Cell migration is assessed using transwell chambers: cells (5×10⁴) are added to upper chambers with RDR 03785, and lower chambers contain 10% FBS or MIF (10 ng/mL) as chemoattractant. Migrated cells are counted after 4-6 h.
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| Animal Protocol |
No animal protocol is published. Generic protocol for MIF inhibitor in LPS-induced inflammation: female C57BL/6 mice (6-8 weeks, n=8/group) receive RDR 03785 (10-50 mg/kg, i.p. or oral) 1 h prior to LPS injection (10-20 mg/kg, i.p.). Blood is collected 2-6 h post-LPS, and serum TNF-alpha, IL-1beta, and IL-6 levels are measured by ELISA. Liver and lung tissues are harvested for qPCR analysis of cytokine mRNA expression and H&E staining for inflammatory cell infiltration. Survival studies (n=20/group) monitor mortality over 5-7 days.
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| ADME/Pharmacokinetics |
No PK data reported. Generic PK for MIF inhibitors: male SD rats or C57BL/6 mice (n=3-4/time point) receive single IV (2-5 mg/kg) or oral (10-30 mg/kg) dose of RDR 03785. Blood samples are collected via jugular vein or tail vein at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, and 24 h. Plasma is separated and analyzed by LC-MS/MS. PK parameters: t1/2 (2-6 h), Cmax (0.5-5 microM), Tmax (0.5-2 h), AUC, CL, Vd, and oral bioavailability (F%). Covalent inhibitors may show prolonged pharmacodynamic effects beyond PK half-life.
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| Toxicity/Toxicokinetics |
No toxicity data reported. Generic acute toxicity study: ICR mice (5/sex/group) receive single oral or i.p. doses of RDR 03785 at 50, 150, 300 mg/kg in 0.5% methylcellulose. Animals are observed for 14 days for mortality, clinical signs (weight loss, piloerection, hunched posture, ataxia), and food/water consumption. At termination, gross necropsy is performed, and major organs (liver, kidney, spleen, heart, lung, brain, GI tract) are collected for histopathological examination. Potential target organs for MIF inhibitors include the immune system and adrenal glands.
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| References | |
| Additional Infomation |
RDR 03785 is a research-grade covalent MIF inhibitor. As a covalent inhibitor, it irreversibly binds to MIF, offering sustained target inhibition. The compound is not FDA-approved and has not entered clinical trials. It is used in laboratory research to study the role of MIF in cancer, inflammation, and immune disorders, and to validate MIF as a therapeutic target. RDR 03785 may also serve as a lead compound for developing MIF-targeted therapies for inflammatory diseases and MIF-dependent cancers.
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| Molecular Formula |
C19H18F3NO4
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|---|---|
| Molecular Weight |
381.35
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| Exact Mass |
381.118
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| CAS # |
289657-30-3
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| PubChem CID |
2725942
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
492
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C2=CC(C(N3CCOCC3)C3=CC=C(C(F)(F)F)C=C3)=C(O)C=C2OC1
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| InChi Key |
AWQPMEGCCWPTRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18F3NO4/c20-19(21,22)13-3-1-12(2-4-13)18(23-5-7-25-8-6-23)14-9-16-17(10-15(14)24)27-11-26-16/h1-4,9-10,18,24H,5-8,11H2
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| Chemical Name |
6-[morpholin-4-yl-[4-(trifluoromethyl)phenyl]methyl]-1,3-benzodioxol-5-ol
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 83.33 mg/mL (218.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6223 mL | 13.1113 mL | 26.2226 mL | |
| 5 mM | 0.5245 mL | 2.6223 mL | 5.2445 mL | |
| 10 mM | 0.2622 mL | 1.3111 mL | 2.6223 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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