Inhibitor GW0742 CAS 317318-84-6 Umgubo omhlophe
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Ukusetyenziswa
I-Andarine (S-4) yi-arylpropionamide-derived compound [S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide] kuqala ichazwe nguYin et al.ukuba ibe yimodyuli ekhethiweyo ye-androgen receptor (SARM).I-Andarine (S-4) iboniswe yi-in vitro kunye nezifundo ze-vivo ukuba ibe yi-agonist esebenzayo ye-anabolic, ngaphandle kwemiphumo emibi ehlala ihambelana ne-anabolic-androgenic steroids, ehambelana ngokuyintloko ne-substrate affinity ye-5α-reductase ukuvelisa i-DHT kwi-prostate.
Umsebenzi we-pharmacological we-atarine ucebisa amandla amakhulu e-andarine ekuphuhliseni ii-SARM ezifumanekayo zonyango, ezibonelela ngeenzuzo ezizodwa zonyango ngaphezu kwabalingane babo be-steroidal kunye nethuba elimnandi lokulawula ngokwahlukileyo iziphumo ze-androgen kwiintlobo ezahlukeneyo zezicubu ekujoliswe kuzo, ngoko ke ukunciphisa ukuphazamiseka kokuqhelekileyo. .Ke, i-atarine inesithembiso kwizilingo eziphambili zeklinikhi ezijolise ekuphatheni izifo ezinxulumene neminyaka kunye nokuchasana neempawu zezifo ezinzima ezifana ne-sarcopenia kunye ne-cachexia yomhlaza.
I-Andarine yinto ekhethiweyo ekhethiweyo ye-androgen receptor (AR) kunye ne-Ki ye-4 nM.I-Andarine ibonisa umsebenzi we-anabolic onamandla kwaye osebenzayo kwaye ukhokelela ekukhuthazeni okuxhomekeke kwithamo lokukhula kwi-prostate, i-seminal vesicles, ngokulandelanayo.I-Andarine ineempawu ezinokuthi zibe ne-antiosteoporotic.
I-Andarine (eyayibizwa ngokuba yi-GTx-007; S-4; GTx007; S4) yi-agonist yomlomo kunye ne-non-steroidal androgen receptor (AR), ngokukodwa i-androgen receptor modulator (SARM), enokuba luncedo ekuchithekeni kwemisipha. kunye ne-osteoporosis.Ivula i-AR nge-Ki ye-4 nM kwaye ikhethe izicubu kumalungu e-anabolic.I-Andarine iphandwa ukunyanga iimeko ezinjengokonakala kwezihlunu, i-osteoporosis kunye ne-benign prostatic hypertrophy.Kwimodeli yezilwanyana ze-benign prostatic hypertrophy, i-andarine yaboniswa ukunciphisa ubunzima be-prostate kunye nokusebenza okufanayo kwi-finasteride, kodwa ngaphandle kokuvelisa nayiphi na ukunciphisa ubunzima be-muscle okanye i-anti-androgenic side effects.
Iinkcukacha
igama eliqhelekileyo | I-SARM S4 | Igama lesiNgesi | IAndarine |
Inombolo yeCAS | 401900-40-1 | ubunzima bemolekyuli | 441.358 |
ukuxinana | 1.5±0.1 g/cm3 | indawo ebilayo | 698.7±55.0 °C kwi-760 mmHg |
ifomula yemolekyuli | C 19 H 18 F 3 N 3 O 6 | Indawo yokunyibilika | 70-74ºC |
PSA | 133.48000 | Indawo yokuflasha | 376.4±31.5 °C |
LogP | 4.01 | uxinzelelo lomphunga | 0.0±2.3 mmHg ku-25°C |