| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
The HEK293-DDR1b cells treated with VU6015929 (Compound 7e; 4-100 nM; 24 hours) showed a dose-dependent inhibition of collagen I-induced DDR1 phosphorylation. According to a study of the phosphorylated DDR1/total DDR1 ratio, VU6015929's IC50 is 0.7078 nM [1].
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|---|---|
| ln Vivo |
VU6015929 (Compound 7e) was further examined in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK trial in 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 demonstrates good in vitro:in vivo correlation (IVIC), has moderate in vivo clearance (CLp = 34.2 mL/min/kg), a half-life of approximately 3 hours, and a moderate volume of distribution at steady state (Vss = 4.3 L) /kg) and 12.5% oral bioavailability with a quick Tmax (0.75 hours) [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293-DDR1b Cell Tested Concentrations: 4 nM, 20 nM, 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibits collagen I-induced DDR1 phosphorylation in a dose-dependent manner. Dramatically inhibits the production of type IV collagen. |
| References |
| Molecular Formula |
C24H19F4N5O2
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|---|---|
| Molecular Weight |
485.4336
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| Exact Mass |
485.147
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| CAS # |
2442597-56-8
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| PubChem CID |
145925694
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| Appearance |
White to yellow solid powder
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| Density |
1.37±0.1 g/cm3(Predicted)
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| Boiling Point |
553.3±50.0 °C(Predicted)
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
699
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IZKVIUJIUTXIRH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19F4N5O2/c1-33-8-7-21(32-33)17-9-15(12-29-14-17)13-30-22-10-16(5-6-20(22)25)23(34)31-18-3-2-4-19(11-18)35-24(26,27)28/h2-12,14,30H,13H2,1H3,(H,31,34)
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| Chemical Name |
4-fluoro-3-[[5-(1-methylpyrazol-3-yl)pyridin-3-yl]methylamino]-N-[3-(trifluoromethoxy)phenyl]benzamide
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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 : ~250 mg/mL (~515.01 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.28 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 (4.28 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 | 2.0600 mL | 10.3001 mL | 20.6003 mL | |
| 5 mM | 0.4120 mL | 2.0600 mL | 4.1201 mL | |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0600 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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