| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
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| Targets |
VUN28691 targets p38α mitogen-activated protein kinase (MAPK), a member of the MAPK family that plays critical roles in cellular responses to stress, inflammation, and differentiation. p38α is involved in the regulation of pro-inflammatory cytokine production and is a validated target for inflammatory diseases. VUN28691 is a selective inhibitor of p38α and can block myoblast differentiation, indicating its role in muscle cell development.
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| ln Vitro |
In vitro, VUN28691 is a selective inhibitor of p38α MAPK. It can block myoblast differentiation, demonstrating its functional activity in cell-based systems. The compound is used as a research tool to study p38α-mediated signaling pathways and their roles in inflammation, stress responses, and cell differentiation. Quantitative in vitro data such as IC50 values are not readily available from publicly accessible sources.
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| ln Vivo |
In vivo activity of VUN28691 has not been extensively reported. As a p38α inhibitor, it may have potential for treating p38α-mediated diseases, including inflammatory conditions. The compound's ability to inhibit p38α suggests potential applications in inflammatory disease research. However, detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for VUN28691 typically involves measuring its inhibition of p38α kinase activity. The compound is incubated with recombinant p38α enzyme in the presence of ATP and a peptide substrate. Kinase activity is measured using a luminescent or fluorescence-based assay (e.g., ADP-Glo or TR-FRET) to determine IC50 values. Selectivity profiling against other MAPK family members can be performed to confirm specificity for p38α.
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| Cell Assay |
The in vitro cell-based assay for VUN28691 involves culturing cells that respond to p38α signaling, such as myoblasts or macrophages. Cells are treated with VUN28691 at various concentrations, and p38α activity is assessed by measuring phosphorylation of downstream substrates such as MAPKAPK2 or HSP27 by Western blot. Myoblast differentiation can be assessed by measuring expression of differentiation markers or by morphological analysis. Cytokine production in stimulated macrophages can also be measured to assess inhibition of p38α-mediated inflammation.
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| Animal Protocol |
In vivo animal studies for VUN28691 have not been extensively reported. If conducted, such studies might involve mouse models of inflammatory diseases, where VUN28691 is administered orally or intraperitoneally and inflammatory markers are measured. Standard protocols for p38α inhibitor evaluation would be employed. No specific data are available from publicly accessible sources.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of VUN28691 have not been extensively characterized. As a small molecule with a molecular weight of 297.37 and a molecular formula of C19H20FNO, it is expected to have moderate oral bioavailability. The compound is a solid powder with a purity of ≥98% and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of VUN28691 has not been systematically evaluated. As a research compound targeting p38α, its primary safety concerns would relate to on-target effects on immune function and inflammation. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available from publicly accessible sources.
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| References | |
| Additional Infomation |
VUN28691 is a research compound and has not been approved for clinical use. It is a selective inhibitor of p38α MAPK, also known as "p38α inhibitor 3" or Compound G7. The compound can block myoblast differentiation and is used for research into p38α-mediated conditions. VUN28691 was first reported in patent WO2000012074 and is available for research purposes only.
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| Molecular Formula |
C19H20FNO
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| Molecular Weight |
297.373
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| Exact Mass |
297.152
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| Elemental Analysis |
C, 76.74; H, 6.78; F, 6.39; N, 4.71; O, 5.38
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| CAS # |
260428-69-1
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| Related CAS # |
260428-69-1;
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
443.9±28.0 °C at 760 mmHg
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| Flash Point |
222.3±24.0 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
3.65
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| InChi Key |
VALGZDLHWXYOBZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20FNO/c20-18-8-6-17(7-9-18)19(22)21-12-10-16(11-13-21)14-15-4-2-1-3-5-15/h1-9,16H,10-14H2
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| Chemical Name |
Methanone, (4-fluorophenyl)[4-(phenylmethyl)-1-piperidinyl]-
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| Synonyms |
p38α inhibitor 3
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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) |
DMSO : ~125 mg/mL (~420.35 mM)
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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 | 3.3628 mL | 16.8141 mL | 33.6281 mL | |
| 5 mM | 0.6726 mL | 3.3628 mL | 6.7256 mL | |
| 10 mM | 0.3363 mL | 1.6814 mL | 3.3628 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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