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| 5mg |
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| 25mg |
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Purity: ≥98%
PF-06471553 (PF06471553) is a novel, potent, selective and orally bioavailable monoacylglycerol acyltransferase 3 (MGAT3) inhibitor with the potential to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis. It inhibits MGAT3 with an IC50 of 92 nM. PF-06471553 selectively inhibits MGAT3 with high in vitro potency and cell efficacy. Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis. Monoacylglycerol acyltransferase 3 (MGAT3) is an integral membrane enzyme that catalyzes the acylation of both monoacylglycerol (MAG) and diacylglycerol (DAG) to generate DAG and TAG, respectively.
| ln Vitro |
With an IC50 of 92 nM, PF-06471553 (6f) is a strong and selective inhibitor of monoacylglycerol acyltransferase 3 (MGAT3) that exhibits selectivity for MGAT3 over DGAT1 (IC50, >50 μM) and DGAT2 (IC50, >50 μM) by more than 160 times in vitro. MGAT1 (IC50, 14.9 μM), MGAT2 (IC50, 19.8 μM), and >100 μM. With an IC50 of 205 nM (pIC50, 6.69), PF-06471553 demonstrates inhibitory efficacy against MGAT3 in HEK-293 cells[1].
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| ln Vivo |
In addition to DGAT1 and DGAT2 inhibitors, PF-06471553 (200 mg/kg, oral) demonstrated significant inhibitory effects on glycerol-d5 incorporation into triolein in hMGAT3 mice, while having no effect on WT mice [1].
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| References |
[1]. Huard K, et al. Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72.
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| Molecular Formula |
C23H25N5O4S
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| Molecular Weight |
467.54070353508
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| CAS # |
1808094-07-6
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| SMILES |
O=S(C1=CC2=C(CN(C(CC3=CC=CC(OC)=C3)=O)C2)C=C1)(NC4=NN(C5CCC5)N=C4)=O
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| InChi Key |
GRXCLNMCJWKTAT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N5O4S/c1-32-20-7-2-4-16(10-20)11-23(29)27-14-17-8-9-21(12-18(17)15-27)33(30,31)26-22-13-24-28(25-22)19-5-3-6-19/h2,4,7-10,12-13,19H,3,5-6,11,14-15H2,1H3,(H,25,26)
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| Chemical Name |
N-(2-cyclobutyl-2H-1,2,3-triazol-4-yl)-2-(2-(3-methoxyphenyl)acetyl)isoindoline-5-sulfonamide
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| Synonyms |
PF-06471553; PF-6471553; PF 06471553; PF 6471553; PF06471553; PF6471553.
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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 : ≥ 150 mg/mL (~320.83 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1389 mL | 10.6943 mL | 21.3885 mL | |
| 5 mM | 0.4278 mL | 2.1389 mL | 4.2777 mL | |
| 10 mM | 0.2139 mL | 1.0694 mL | 2.1389 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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