| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In HFL-1 cells, R-268712 (3, 10, 30, 100, 300 nM; 1 h) suppresses Smad3 phosphorylation in a dose-dependent manner with an IC50 of 10.4 nM [1]. Without affecting the proliferation of HFL-1 cells, R-268712 (3, 10, 30, 100, and 300 nM; 72 h) suppresses the myofibroblast transdifferentiation (MTD) of fibroblasts in a dose-dependent manner [1].
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| ln Vivo |
In the UUO model, R-268712 (1, 3, 10 mg/kg; oral; once daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner [2]. In a Thy1 nephritis model, R-268712 (0.3, 1, 3, 10 mg/kg; oral; single dose) demonstrated renoprotective effects (improvement and maintenance of renal function and inhibition of glomerular function) at 1 mg/kg [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HFL-1 Cell Tested Concentrations: 3, 10, 30, 100, 300 nM Incubation Duration: 1 or 72 hrs (hours) Experimental Results: Inhibited the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 incubation 1 hrs (hours) are nM. Inhibited myofibroblast transdifferentiation (MTD), but not cell growth, of fibroblasts in a dose-dependent manner after 72 hrs (hours) of incubation. |
| Animal Protocol |
Animal/Disease Models: Male WKY/Hos rat [2]. Strength: 0.3, 1, 3 and 10 mg/kg
Route of Administration: Oral; single. Experimental Results: 1.19 pharmacokinetic/PK/PK parameters of R-268712 in male WKY/Hos rats (n=4)[2]. PO (0.3 mg/kg) PO (1 mg/kg) PO (3 mg/kg) PO (10 mg/kg) AUC0-24 (μg·h/mL) 0.075 0.28 1.6 8.2 Animal/Disease Models: Male Col1a1-Luc Tg Rats (10 to 14 weeks old; UUO model; n=5-6) [2]. Doses: 1, 3, 10 mg/kg Doses: po (po (oral gavage)) one time/day for 3 days. Experimental Results: Inhibition of renal luciferase activity in a dose-dependent manner. Animal/Disease Models: Male WKY/Hos rats (4 weeks old; Thy1 nephritis model; n=7) [2]. Doses: 0.3, 1 mg/kg Route of Administration: Oral; one time/day for 33 days. Experimental Results: Proteinuria on day 21 (suppression continued until day 28) and serum creatinine levels (dose 1 mg/kg) were Dramatically diminished. At 1 mg/kg, it Dramatically inhibits glomerulosclerosis by 28% and reduces the increase in hydroxyproline content. 1 mg/kg inhibits the activation of mesangial parenchymal cells and the damage of podocytes on the basis |
| References |
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| Molecular Formula |
C20H18FN5O
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|---|---|
| Molecular Weight |
363.39
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| Exact Mass |
363.149
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| CAS # |
879487-87-3
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| PubChem CID |
11703284
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
576.8±50.0 °C at 760 mmHg
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| Flash Point |
302.7±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
2.79
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
483
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JQGOCCALXFSRHZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18FN5O/c1-13-3-2-4-19(24-13)20-17(11-22-25-20)14-5-6-18(21)16(9-14)15-10-23-26(12-15)7-8-27/h2-6,9-12,27H,7-8H2,1H3,(H,22,25)
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| Chemical Name |
2-[4-[2-fluoro-5-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]phenyl]pyrazol-1-yl]ethanol
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| Synonyms |
R-268712 R268712 R 268712
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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 (~343.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.72 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 (5.72 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 (5.72 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 | 2.7519 mL | 13.7593 mL | 27.5186 mL | |
| 5 mM | 0.5504 mL | 2.7519 mL | 5.5037 mL | |
| 10 mM | 0.2752 mL | 1.3759 mL | 2.7519 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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