Chemistry:TFM-4AS-1
 | |
| Clinical data | |
|---|---|
| Other names | N-[2-(Trifluoromethyl)phenyl]-3-oxo-4-aza-4-methyl-5α-androst-1-en-17α-carboxamide |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| Chemical and physical data | |
| Formula | C27H33F3N2O2 |
| Molar mass | 474.568 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
TFM-4AS-1 is a dual selective androgen receptor modulator (SARM) and 5α-reductase inhibitor.[1][2] It is a potent and selective partial agonist (Emax = 55%) of the androgen receptor (IC50 = 30 nM) and inhibitor of 5α-reductase types I and II (IC50 = 2 and 3 nM, respectively).[1][2] TFM-4AS-1 shows tissue-selective androgenic effects; it promotes the accumulation of bone and muscle mass and has reduced effects in reproductive tissues and sebaceous glands.[2] In an animal study, TFM-4AS-1 stimulated sebaceous gland formation only 31% as much as dihydrotestosterone (DHT) at doses that were as anabolic or more so than DHT.[3][2] In addition, TFM-4AS-1 only weakly promoted growth of the prostate gland and it partially antagonized the actions of DHT in the seminal vesicles and endogenous androgens in the prostate gland.[2] Structurally, TFM-4AS-1 is a 4-azasteroid.[1] A structurally related and more advanced version of TFM-4AS-1, MK-0773, was developed and pursued for potential pharmaceutical use.[3]
See also
References
- ↑ 1.0 1.1 1.2 "4-Methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-N-aryl-carboxamides: an approach to combined androgen blockade [5alpha-reductase inhibition with androgen receptor binding in vitro]". J. Steroid Biochem. Mol. Biol. 60 (5–6): 303–9. 1997. doi:10.1016/s0960-0760(96)00199-9. PMID 9219921.
- ↑ 2.0 2.1 2.2 2.3 2.4 "Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands". J. Biol. Chem. 284 (52): 36367–76. 2009. doi:10.1074/jbc.M109.049734. PMID 19846549.
- ↑ 3.0 3.1 "Deciphering the selective androgen receptor modulators paradigm". Expert Opin Drug Discov 8 (2): 191–218. February 2013. doi:10.1517/17460441.2013.741582. PMID 23231475.
 |  |
