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YK-11 is a synthetic steroidal selective androgen receptor modulator (SARM).[1][2] It is a gene-selective partial agonist of the androgen receptor (AR) and does not induce the physical interaction between the NTD/AF1 and LBD/AF2 (known as the N/C interaction), which is required for full transactivation of the AR.[1][2] The drug has anabolic activity in vitro in C2C12 myoblasts and shows greater potency than dihydrotestosterone (DHT) in this regard.[2] It has been investigated as a potential treatment for sepsis-induced muscle wasting in animal studies.[3]

See also

References

  1. ^ a b Kanno Y, Hikosaka R, Zhang SY, Inoue Y, Nakahama T, Kato K, et al. (2011). "(17α,20E)-17,20-[(1-methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11) is a partial agonist of the androgen receptor". Biological & Pharmaceutical Bulletin. 34 (3): 318–323. doi:10.1248/bpb.34.318. PMID 21372378.
  2. ^ a b c Kanno Y, Ota R, Someya K, Kusakabe T, Kato K, Inouye Y (2013). "Selective androgen receptor modulator, YK11, regulates myogenic differentiation of C2C12 myoblasts by follistatin expression". Biological & Pharmaceutical Bulletin. 36 (9): 1460–1465. doi:10.1248/bpb.b13-00231. PMID 23995658.
  3. ^ Lee SJ, Gharbi A, Shin JE, Jung ID, Park YM (March 2021). "Myostatin inhibitor YK11 as a preventative health supplement for bacterial sepsis". Biochemical and Biophysical Research Communications. 543: 1–7. doi:10.1016/j.bbrc.2021.01.030. PMID 33588136.
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