| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
CPSI-1306 targets macrophage migration inhibitory factor (MIF), a pro-inflammatory cytokine involved in various immune responses and inflammatory processes. It acts as an antagonist, inhibiting the activity of MIF. By blocking MIF, it modulates inflammatory responses and has potential therapeutic applications in inflammatory diseases, cancer, and other conditions.
|
|---|---|
| ln Vitro |
In vitro, CPSI-1306 is an antagonist of MIF. It inhibits the activity of this pro-inflammatory cytokine. However, specific in vitro activity data, such as IC50 values, are not well-documented in the available literature. Its activity is primarily demonstrated in in vivo models.
|
| ln Vivo |
Blood glucose levels significantly dropped in mice given CPSI-1306, and this was correlated with lower levels of inflammatory cytokines in the serum. Anticipatedly, mice under vehicle treatment developed non-insulin-dependent diabetic macular disease (NIDDM), typified by elevated serum levels of glucose and inflammatory cytokines. Furthermore, they demonstrated the efficacious treatment of this illness by orally accessible CPSI-1306 [1]. One can witness CPSI-1306-induced keratinocyte death as early as half an hour following a single UVB exposure. At6,24, and 48 hours following UVB exposure, mice treated with CPSI-1306 had significantly higher expression of cleaved caspase-3 as compared to mice treated with vehicle. UVB-induced acute inflammation and keratinocyte DNA damage can both be reduced by CPSI-1306 [2].
In vivo, CPSI-1306 has shown significant effects in a mouse model of UVB-induced skin cancer. At a dose of 20 mg/kg per day, it decreases skin thickness and myeloperoxidase (MPO) activity, induces keratinocyte apoptosis, and reduces papilloma formation and progression to micro-invasive squamous cell carcinoma (SCC). It also reduces acute UVB-induced keratinocyte DNA damage and UVB-induced acute inflammation. Additionally, in mice, CPSI-1306 decreases blood glucose levels and can be effective in treating non-insulin-dependent diabetes mellitus (NIDDM). |
| Enzyme Assay |
CPSI-1306 is evaluated in cell-free assays to measure its ability to inhibit MIF. However, specific enzymatic or receptor binding assays are not well-documented. Its purity and identity can be confirmed using HPLC and NMR analysis. The compound's activity is typically assessed in cell-based and in vivo systems.
|
| Cell Assay |
CPSI-1306 is assessed in cell-based assays to study its effects on MIF activity and inflammation. Cells are treated with CPSI-1306, and the production of inflammatory cytokines and other markers of MIF activity are measured. However, specific cell-based assay protocols are not extensively documented.
|
| Animal Protocol |
CP-424174 is administered orally in animal models to evaluate its effects on inflammation and cancer. It has been studied in a mouse model of UVB-induced skin cancer and in models of diabetes. Efficacy is assessed by measuring skin thickness, MPO activity, papilloma formation, blood glucose levels, and inflammatory cytokine levels.
|
| ADME/Pharmacokinetics |
CPSI-1306 has a molecular formula of C15H16F2N2O3 and a molecular weight of 310.30. Its CAS number is 1309793-47-2. The compound is a solid. It is soluble in DMSO. It should be stored at -20°C. It is also known as (±)-CPSI-1306.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CPSI-1306. The compound is for research use only and is not intended for human therapeutic use. It is an orally available MIF antagonist used to study the role of MIF in inflammation, cancer, and diabetes.
|
| References | |
| Additional Infomation |
CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF). It is also known as (±)-CPSI-1306. It reduces UVB-induced skin damage and inflammation, and has shown efficacy in models of diabetes. The compound is not approved for clinical use.
|
| Molecular Formula |
C15H16F2N2O3
|
|---|---|
| Molecular Weight |
310.3
|
| Exact Mass |
310.112
|
| CAS # |
1309793-47-2
|
| PubChem CID |
59723793
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
453.3±55.0 °C at 760 mmHg
|
| Flash Point |
227.9±31.5 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.591
|
| LogP |
1.27
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
22
|
| Complexity |
441
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1COCCN1C(=O)CC2CC(=NO2)C3=C(C=C(C=C3)F)F
|
| InChi Key |
GUWOSEVHCSNYFK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H16F2N2O3/c16-10-1-2-12(13(17)7-10)14-8-11(22-18-14)9-15(20)19-3-5-21-6-4-19/h1-2,7,11H,3-6,8-9H2
|
| Chemical Name |
2-[3-(2,4-difluorophenyl)-4,5-dihydro-1,2-oxazol-5-yl]-1-morpholin-4-ylethanone
|
| Synonyms |
CPSI1306; CPSI 1306; CPSI-1306
|
| 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) |
DMSO : ~6 mg/mL (~19.34 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (1.93 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 6.0 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: ≥ 0.6 mg/mL (1.93 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 6.0 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: ≥ 0.6 mg/mL (1.93 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 | 3.2227 mL | 16.1134 mL | 32.2269 mL | |
| 5 mM | 0.6445 mL | 3.2227 mL | 6.4454 mL | |
| 10 mM | 0.3223 mL | 1.6113 mL | 3.2227 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
