| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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PF-06424439 Mesylate, the mesylate salt of PF06424439, is a novel and potent inhibitor of diacylglycerol acyltransferase 2 (DGAT2, IC50 = 14 nM) with lipid lowering effects.
| Targets |
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| ln Vivo |
Mice (Ldlr-/-) treated with PF-06424439 methanesulfonate (oral; 60 mg/kg/day; for 3 days) have lower plasma TG and cholesterol levels as well as lower circulating lipid levels [1]. Rats administered PF-06424439 methanesulfonate (iv; 1 mg/kg) intravenously show a short half-life, moderate steady-state volume of distribution (Vdss), and moderate clearance [1].
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| Animal Protocol |
Animal/Disease Models: Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1]
Doses: 60 mg/kg Route of Administration: Po; daily; for 3 days Experimental Results: decreased plasma TG and cholesterol levels and diminished nonsignificant in circulating lipids. Animal/Disease Models: Male Wistar-Han rats[1] Doses: 1 mg/kg Route of Administration: Iv Experimental Results: demonstrated moderate clearance and a short half-life with t1/2=1.39 h. |
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| References |
[1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85.
[2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010. |
| Molecular Formula |
C23H30CLN7O4S
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|---|---|
| Molecular Weight |
536.04
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| CAS # |
1469284-79-4
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| Related CAS # |
PF-06424439;1469284-78-3
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| SMILES |
O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6.CS(=O)(O)=O
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| InChi Key |
ZSTFDNQQOJUJFL-XFULWGLBSA-N
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| InChi Code |
InChI=1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-281-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27)1H3,(H,2,3,4)/t15-/m1./s1
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| Chemical Name |
[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate
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| Synonyms |
PF06424439 Mesylate PF 06424439 Mesylate PF-06424439 Mesylate
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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 (~466.37 mM)
H2O : ~50 mg/mL (~93.27 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.88 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 (3.88 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 (3.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (93.27 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8655 mL | 9.3277 mL | 18.6553 mL | |
| 5 mM | 0.3731 mL | 1.8655 mL | 3.7311 mL | |
| 10 mM | 0.1866 mL | 0.9328 mL | 1.8655 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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