| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
VAF347 (VAF-347) is a novel and potent aryl hydrocarbon receptor (AhR) agonist which is cell permeable and has highly affinity against aryl hydrocarbon receptor (AhR). It has anti-inflammatory effects by inducing AhR signaling and nhibiting the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors.
| ln Vitro |
Treatment with VAF347 (0.01–20 μM; 48–72 hours; HL-60 cells) improves the cell life cycle triggered by retinoic acid [1]. Treatment with VAF347 (20 μM; 48 h; HL-60 cells) improves the cell cycle initiated by retinoic acid[1]. expression of AhR, Lyn, Vav1, c-Cbl, and p47phox that is stimulated by acid. The MM1 cells' IL-4+ GM-CSF-induced IL-6 production is inhibited by Fgr with c-Cbl, CD38, and pS259c-Raf and AhR with c-Cbl and VAF347; the IC50 is roughly 5 nM[2]. Several responses appear to be amplified in the signalosome.
|
|---|---|
| ln Vivo |
Total serum IgE levels in wild-type mice treated with VAF347 were significantly lower than in animals given vehicle therapy. Significantly less IL-5 was present in the mutant alveolar fluid. VAF347 can cause allergic lung inflammation in vivo, although AhR-deficient animals are not susceptible to this effect [2].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: HL-60 Cell Tested Concentrations: 10 nM, 100 nM, 1 μM, 10 μM, 20 μM Incubation Duration: 48 hrs (hours) or 72 hrs (hours) Experimental Results: Enhanced retinoic acid-induced G1/0 cell cycle Stagnation. Western Blot Analysis[1] Cell Types: HL-60 Cell Tested Concentrations: 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Enhanced retinoic acid-induced expression of AhR, Lyn, Vav1 and c-Cbl, and p47phox. |
| References |
|
| Molecular Formula |
C₁₇H₁₁CLF₃N₃
|
|---|---|
| Molecular Weight |
349.74
|
| Exact Mass |
349.059
|
| CAS # |
574759-62-9
|
| PubChem CID |
10172275
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.632
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
399
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XTKUZTBZRIJTFR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H11ClF3N3/c18-13-3-1-2-11(10-13)15-8-9-22-16(24-15)23-14-6-4-12(5-7-14)17(19,20)21/h1-10H,(H,22,23,24)
|
| Chemical Name |
4-(3-chlorophenyl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine
|
| Synonyms |
VAF 347 VAF-347
|
| 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 : ~31.25 mg/mL (~89.35 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.95 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8593 mL | 14.2963 mL | 28.5927 mL | |
| 5 mM | 0.5719 mL | 2.8593 mL | 5.7185 mL | |
| 10 mM | 0.2859 mL | 1.4296 mL | 2.8593 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
