SR 1664CAS# 1338259-05-4 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 1338259-05-4 | SDF | Download SDF |
| PubChem ID | 53239854 | Appearance | Powder |
| Formula | C33H29N3O5 | M.Wt | 547.6 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol | ||
| Chemical Name | 2-[4-[[2,3-dimethyl-5-[[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acid | ||
| SMILES | CC1=C(N(C2=C1C=C(C=C2)C(=O)NC(C)C3=CC=C(C=C3)[N+](=O)[O-])CC4=CC=C(C=C4)C5=CC=CC=C5C(=O)O)C | ||
| Standard InChIKey | IIJDFXNUWZTHIM-NRFANRHFSA-N | ||
| Standard InChI | InChI=1S/C33H29N3O5/c1-20-22(3)35(19-23-8-10-25(11-9-23)28-6-4-5-7-29(28)33(38)39)31-17-14-26(18-30(20)31)32(37)34-21(2)24-12-15-27(16-13-24)36(40)41/h4-18,21H,19H2,1-3H3,(H,34,37)(H,38,39)/t21-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Antidiabetic agent; binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity. Does not inhibit Cdk5-dependent phosphorylation of Rb. Reduces fasting insulin levels and improves insulin sensitivity in a mouse model of diabetes. |
SR 1664 Dilution Calculator
SR 1664 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8262 mL | 9.1308 mL | 18.2615 mL | 36.523 mL | 45.6538 mL |
| 5 mM | 0.3652 mL | 1.8262 mL | 3.6523 mL | 7.3046 mL | 9.1308 mL |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8262 mL | 3.6523 mL | 4.5654 mL |
| 50 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.7305 mL | 0.9131 mL |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.3652 mL | 0.4565 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Antidiabetic actions of a non-agonist PPARgamma ligand blocking Cdk5-mediated phosphorylation.[Pubmed:21892191]
Nature. 2011 Sep 4;477(7365):477-81.
PPARgamma is the functioning receptor for the thiazolidinedione (TZD) class of antidiabetes drugs including rosiglitazone and pioglitazone. These drugs are full classical agonists for this nuclear receptor, but recent data have shown that many PPARgamma-based drugs have a separate biochemical activity, blocking the obesity-linked phosphorylation of PPARgamma by Cdk5. Here we describe novel synthetic compounds that have a unique mode of binding to PPARgamma, completely lack classical transcriptional agonism and block the Cdk5-mediated phosphorylation in cultured adipocytes and in insulin-resistant mice. Moreover, one such compound, SR1664, has potent antidiabetic activity while not causing the fluid retention and weight gain that are serious side effects of many of the PPARgamma drugs. Unlike TZDs, SR1664 also does not interfere with bone formation in culture. These data illustrate that new classes of antidiabetes drugs can be developed by specifically targeting the Cdk5-mediated phosphorylation of PPARgamma.
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