TFM-4AS-1Selective androgen receptor modulator (SARM) CAS# 188589-61-9 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 188589-61-9 | SDF | Download SDF |
| PubChem ID | 10277123 | Appearance | Powder |
| Formula | C27H33F3N2O2 | M.Wt | 474.56 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO and to 10 mM in ethanol | ||
| Chemical Name | (1S,3aS,3bS,5aR,9aR,9bS,11aS)-6,9a,11a-trimethyl-7-oxo-N-[2-(trifluoromethyl)phenyl]-2,3,3a,3b,4,5,5a,9b,10,11-decahydro-1H-indeno[5,4-f]quinoline-1-carboxamide | ||
| SMILES | CC12CCC3C(C1CCC2C(=O)NC4=CC=CC=C4C(F)(F)F)CCC5C3(C=CC(=O)N5C)C | ||
| Standard InChIKey | YFBLEKKYWFJKBP-JZFZSVFHSA-N | ||
| Standard InChI | InChI=1S/C27H33F3N2O2/c1-25-14-12-18-16(8-11-22-26(18,2)15-13-23(33)32(22)3)17(25)9-10-20(25)24(34)31-21-7-5-4-6-19(21)27(28,29)30/h4-7,13,15-18,20,22H,8-12,14H2,1-3H3,(H,31,34)/t16-,17-,18-,20+,22+,25-,26+/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 | Potent selective androgen receptor modulator (SARM) (IC50 = 30 nM). Steroidal compound. Exhibits limited effects on reproductive tissues and sebaceous glands; does not repress AP-1-sensitive MMP-1 reporter. Inhibits 5α-reductase type I and II (IC50 values are 2 and 3 nM respectively). |
TFM-4AS-1 Dilution Calculator
TFM-4AS-1 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1072 mL | 10.5361 mL | 21.0722 mL | 42.1443 mL | 52.6804 mL |
| 5 mM | 0.4214 mL | 2.1072 mL | 4.2144 mL | 8.4289 mL | 10.5361 mL |
| 10 mM | 0.2107 mL | 1.0536 mL | 2.1072 mL | 4.2144 mL | 5.268 mL |
| 50 mM | 0.0421 mL | 0.2107 mL | 0.4214 mL | 0.8429 mL | 1.0536 mL |
| 100 mM | 0.0211 mL | 0.1054 mL | 0.2107 mL | 0.4214 mL | 0.5268 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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Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.[Pubmed:19846549]
J Biol Chem. 2009 Dec 25;284(52):36367-76.
Androgen replacement therapy is a promising strategy for the treatment of frailty; however, androgens pose risks for unwanted effects including virilization and hypertrophy of reproductive organs. Selective Androgen Receptor Modulators (SARMs) retain the anabolic properties of androgens in bone and muscle while having reduced effects in other tissues. We describe two structurally similar 4-aza-steroidal androgen receptor (AR) ligands, Cl-4AS-1, a full agonist, and TFM-4AS-1, which is a SARM. TFM-4AS-1 is a potent AR ligand (IC(50), 38 nm) that partially activates an AR-dependent MMTV promoter (55% of maximal response) while antagonizing the N-terminal/C-terminal interaction within AR that is required for full receptor activation. Microarray analyses of MDA-MB-453 cells show that whereas Cl-4AS-1 behaves like 5alpha-dihydrotestosterone (DHT), TFM-4AS-1 acts as a gene-selective agonist, inducing some genes as effectively as DHT and others to a lesser extent or not at all. This gene-selective agonism manifests as tissue-selectivity: in ovariectomized rats, Cl-4AS-1 mimics DHT while TFM-4AS-1 promotes the accrual of bone and muscle mass while having reduced effects on reproductive organs and sebaceous glands. Moreover, TFM-4AS-1 does not promote prostate growth and antagonizes DHT in seminal vesicles. To confirm that the biochemical properties of TFM-4AS-1 confer tissue selectivity, we identified a structurally unrelated compound, FTBU-1, with partial agonist activity coupled with antagonism of the N-terminal/C-terminal interaction and found that it also behaves as a SARM. TFM-4AS-1 and FTBU-1 represent two new classes of SARMs and will allow for comparative studies aimed at understanding the biophysical and physiological basis of tissue-selective effects of nuclear receptor ligands.
