Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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Targets |
CYP4A11 140 nM (IC50) CYP4F2 40 nM (IC50)
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ln Vitro |
With an IC50 of 29 nM, CYP4A11/CYP4F2-IN-2 (compound 11c) suppresses the synthesis of 20-Hydroxyeicosatetraenoic acid (20-HETE) from arachidonic acid in human renal microsomes[1].
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ln Vivo |
CYP4A11/CYP4F2-IN-2 (compound 11c) suppresses the synthesis of 20-HETE in the rats' kidneys in a dose-dependent manner (0.03-1 mg/kg; single po)[1]. Mice treated with 0.5 mg/kg of CYP4A11/CYP4F2-IN-2 show modest Vdss (763 mL/kg), short T1/2 (0.424 h), and low CL (1430 mL/h/kg)[1]. The study reports that in SD rats, CYP4A11/CYP4F2-IN-2 (1 mg/kg; iv) displays low CL (226 mL/h/kg), moderate Vdss (839 mL/kg), and T1/2 (3.01 h). In SD rats, CYP4A11/CYP4F2-IN-2 (1 mg/kg; po) shows a high bioavailability (97.7%), T1/2 (3.03 h), and Cmax (623 ng/mL[1].
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References |
[1]. Kawamura M, et, al. Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition. J Med Chem. 2022 Nov 10;65(21):14599-14613.
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Molecular Formula |
C16H20N4O2
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Molecular Weight |
300.36
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CAS # |
2126874-77-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(=O)(N1CCC(COC2=CC=C(C3C=CNN=3)N=C2)CC1)C
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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: 25 mg/mL (83.23 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.32 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 25.0 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: ≥ 2.5 mg/mL (8.32 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 25.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3293 mL | 16.6467 mL | 33.2934 mL | |
5 mM | 0.6659 mL | 3.3293 mL | 6.6587 mL | |
10 mM | 0.3329 mL | 1.6647 mL | 3.3293 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.