Testolone (Rad1440 Ua kua)yog ib qho kev xaiv Androgen Revenor Modulator (sarm), Amesternalial tsim los ntawm pob txha tsis zoo, thaum txo cov nqaij tsis sib xws, thaum txo cov nqaij tsis sib xws, thaum txo cov nqaij mos rau ntawm cov nqaij mos xws li cov kua xoo, thiab plaub hau cov hauv paus . nws cov txiaj ntsig Anabolic zoo ib yam li cov khoom siv hluavtaws zoo sib xws thiab muaj peev xwm tshaj tawm kev nyab xeeb dua {4}
Rad1440 kua yog cov kua ntawm cov compound no {1} {{2} {{2} {}}} Txawm li cas los xij, nws Kev Nyab Xeeb Kev Nyab Xeeb Tsis Tau Ua tiav . Lub ntiaj teb kev pom zoo, qaug zog} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb} Lub ntiaj teb {
|
|
|
Rad140 hmoov coa
Cov qauv ntawm cov tshuaj chenisma thiab cov txheej txheem hluavtaws
Tshuaj Yeeb Nkab
Testolone (Rad1440 Ua kua)yog qhov tsis muaj steroidal xaiv Androgen receptor modulator (sarm), nrog molecular qhov hnyav ntawm 393 {}} 826 g / mol. Nws cov qauv tshuaj muaj cov ntsiab lus tseem ceeb hauv qab no:
Oxazole nplhaib
Raws li cov tub ntxhais lub moj khaum, cov nplhaib sib dhos ua rau cov molecuent ntawm cov txiaj ntsig los ntawm kev siv lub zog, thiab ua haujlwm rau kev xaiv tau .
Cyano Group thiab Chlorine Atom
Cov pab pawg Cyano (-cn) ua raws li cov txheej txheem hluav taws xob muaj zog rau kev hloov pauv molecy
HydroxyPropyl sab saw
Muab ib pab pawg polar, txhim kho hydrogen hydring bonding, txhim kho solubility (solubility (solubility), thiab txo cov tshuaj tiv thaiv oxidation (solubility), thiab txo cov tshuaj tiv thaiv oxidation (solubility
Synthesis txheej txheem
Cov synthesis ntawm rad140 xav kom ua tiav ntau cov organic regents . Cov kauj ruam tseem ceeb yog raws li hauv qab no:
Cov Khoom Siv Raw:2-}}} fluoro {}} methylbencomascide thiab HD-}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}} is-huag (hydroxythrooonine).
Cov Kev Mob:Sib xyaw hauv DMOPS, ntxiv cov poov tshuaj Carbonate (K₂CO₃) raws li lub hauv paus, thiab do cov tshuaj tiv thaiv ntawm 75℃.
Khoom:Tebchaw 9 (Purity ntau dua los yog sib npaug ntawm 95%) yog tsim los ntawm acidification, extraction, thiab kem chromatography purification.
Cov Khoom Siv Raw:Compound 9 thiab {{4- Cyanbenzhydrazine .
Cov Kev Mob:Sib tov hauv thf, txias rau -15℃hauv nitrogen tiv thaiv, thiab do cov tshuaj ntxuav cov tshuaj tiv thaiv.
Khoom:Daj Contacound 10 yog tsim (tawm 78%), ua kom tiav 78%), ua kom tiav los ntawm kev lim dej, ntxuav, thiab rhaub}
Silosane tiv thaiv:Rov qab siv tert-butyl dimethyl chalorosilane (tbdmsci) thiab imidazole hauv dichloromsim 10a (tawm 84%) {3} {3}
Iodination neeg:Qhia Iodine atoms los ntawm nucleophilic hloov cov kev coj ua txawv, thiab triethylamine, iodine cibround, thiab kev tsim tawm 104%).
Kev Tiv Thaiv DEA:Tshem cov pab tiv thaiv cov siloxane tiv thaiv siv tetrabutyl fluoride ammonium (TBAF), thiab ntxuav nws cov chromatograph (TMAc), thiab ua kom huv si.
Cov qauv ua kua thiab kev ua kom ruaj khov
Testolone (Rad1440 Ua kua)yuav tsum tau khaws cia rau lub sijhawm ntev los ntawm kev daws qhov kev sib cais thiab qhov sib ntxiv ntawm stabilizers:
Kev xaiv cov kuab:Feem ntau, siab-huv DMOs (ntau dua lossis sib npaug rau kev ua kom tiav ntawm Rad140 (ntau} mg / ml).
Sib tw ntxiv:0 {{. 1% ascorbic acid (vitamin C) lossis 0.01% edylated hydroxisole (BHA) tau ntxiv raws li tus neeg sawv cev chelating los tiv thaiv kev txwv hlau ion.
Kev Cia Cai Cia:
Zam kev kaj
Tsawg kub: nws pom zoo kom khov rau ntawm {{}} Cov neeg nyob ruaj khov rau 1 xyoos ntxiv rau 2 xyoo .
Kev Tswj Xyuas Zoo thiab Nrhiav Kom Tau
Kev ua kom zoo ua kua chromatography (HPLC)
Siv daim C18 (4 .
Kua kua chromatography-mass spectrometry (LC-MS)
Kuaj pom los ntawm electrospray ionization ion hom hom, molecular ion peak (m + h] ⁺), lees paub qhov tseeb ntawm molecular hnyav.
Nuclear Sib Nqus Revelance (NMR)
¹H NMR (400 MHz, DMOPS-D₆) Qhia cov xeeb ntxwv ntawm cov cim (D, Cyas), 7.98 (1,
Cov qauv ua kua thiab kev ua kom ruaj khov
Tsim Kua Ua Kua Tsim
Kev ntsuas kev xaiv
DMOPS (dimethyl sulfoxide): raws li cov tub ntxhais tseem ceeb yuav tsum tau tswj hwm (tsawg dua lossis sib npaug.
Peg400 (Polyethylene Glycol 400): Ib qho kev siv me me yog qhov tsim nyog rau DMOs, nws yuav tsum tau yaj los ntawm cua sov ({} degree).
Xyaw cov kuab tshuaj: DMOPS thiab PEG400 tau sib xyaw hauv 1: 1 piv, uas tuaj yeem ua kom muaj kev sib txuam, thaum txo cov kua dej viscosity thiab kev txhim kho fluplet ntawm cov teeplet {}}
Tshab stabilizer ntxiv
Antioxidant: ntxiv 0 {{. 1% ascorbic acid (vitamin C) lossis Butylated Axidation Decadadation thiab txuas ntxiv rau lub zog txee mus rau 18 lub hlis (ntawm chav tsev kub).
Chelating tus neeg sawv cev: ntxiv 0 {{. 01% edta disodium, xws li Fe³⁺, los tiv thaiv cov catalytic kev ua kom tsis txaus ntseeg.
PHIB REGULATE: Siv phosphate buffer daws (PBS) lossis citrate cov qauv kev puas tsuaj los tswj cov pH nyob rau hauv thaj chaw acidic lossis alkaline {}}
Osmotic Siab Kev Cai
Yog tias cov mis yog siv rau kev txhaj tshuaj lossis kev hloov pauv ntawm lub cev ({} Mauxe}, txo kev txob txob.
Kev Ruaj Ntseg Ua Kom Zoo Dua
Lub teeb ruaj khov txhim kho
Shading ntim: Siv cov raj kub xim av lossis cov ntawv ci txhuas los yog cov ntawv ci txhuas rau ntim kom thaiv 99 {} 9% ntawm ultraviolet lub teeb (UV-A / B).
Lub teeb Stabilizer: ntxiv 0 {.}} an%% d d d,, los ntawm kev tiv thaiv lub cev thiab dawb radical ntes.
Tswj Qhov Kub
Khov cia: Pom zoo kom khov rau ntawm {{}}℃rau cia lossis sib npaug ntawm 5%), thaum lub sijhawm khov kho tuaj yeem txuas ntxiv mus rau 2 xyoo.
Thermal Kev Ntsuas Xyuas Kev Lag Luam: Hauv 40℃pretftated xeem, rad140 kua yog ruaj khov rau ntawm cov qauv sib piv ntawm cov qauv.
Oxidation Dectradation Inhibition
Kev tiv thaiv nitrogen tiv thaiv: thaum sau, qhia cov nitrogen kom tshem tawm cov pa oxygen, txo qhov kev pheej hmoo ntawm oxidation .
Kev ruaj khov: ASCORBIC acid ua ke nrog BHA tuaj yeem txo cov oxidation depradation tus nqi mus rau 24 lub hlis .
Kev tswj kom zoo thiab kev sim cov qauv
Kev ua kom zoo ua kua chromatography (HPLC)
Siv C18 Chromatographic kem (4 {}}}}}}}}} {{{{{{{{{{{{{{{{{nm. Lub sijhawm rad140 yog kwv yees li 8.5 feeb, thiab kev ua kom muaj kev xav tau loj dua lossis sib npaug ntawm 98%.
Kua kua chromatography-mass spectrometry (LC-MS)
Tshawb nrhiav kev siv tshuab hluav taws xob ionization (esi) ion hom, molecular ion peak (m + h] ⁺), lees paub qhov tseeb ntawm molecular hnyav.
Kuaj ruaj khov nrawm
Tso rau hauv 40 Qib / 75 %% ib puag ncig rau 6 lub hlis, coj cov qauv tsawg dua lossis sib npaug ntawm 1 {6}, tus qauv sib luag yog tsim nyog.
Kev Siv Khoom Siv Kom Zoo Dua
Lub tuam txhab biotechnology
Kev sib xyaw: rad 140 10 mg / ml, dmss}}} {{{{5%, Edta Ido 101%.
Cov ntaub ntawv ruaj khov: khaws cia ntawm 25℃rau 12 lub hlis, cov ntsiab lus txo los ntawm 3. 2%, impurities 0.8%; Khaws cia ntawm -20℃rau 24 lub hlis, cov ntsiab lus txo los ntawm 1.5%, impurities 0.3%.
Transdermal thaj qauv
Kev Sau Tseg: Rad 140 5 mg / g, polyacrylate siab-rhiab heev nplaum 80%, titanium dioxide 5% .
Cov ntaub ntawv ruaj khov: thaum khaws cia ntawm 40 hlis rau 3 lub hlis, lub transdle flux tseem nyob ruaj khov nyob rau hauv 12}}}}}}}
Kev tswj kom zoo thiab tshuaj xyuas ib tog
Kev tswj hwm zoo ntawmTestolone (Rad1440 Ua kua)yuav tsum tsom rau peb yam tseem ceeb: kev coj dawb huv, kev ruaj khov tswj {}} {{.} Cov hauv qab no yog kev tswj hwm tshwj xeeb thiab nrhiav txoj hauv kev:
Kev Kuaj Purity Purity
Kev ua kom zoo ua kua chromatography (HPLC)
Txoj kev: Siv C18 kem (4 {}}}}}}}}}
Txheem: Lub sijhawm rad140 yog kwv yees li ntawm PinE 5 feeb, thiab cov khoom siv tsis zoo ntxiv (xws li cov khoom siv hluavtaws ntxiv lossis cov khoom lag luam).
Daim Ntawv Thov: Tsim nyog rau kev ntsuam xyuas sai sai ntawm kev coj dawb huv, thiab yog qhov feem ntau siv cov qauv hauv kev tswj kom zoo .
Kua kua chromatography-mass spectrometry (LC-MS)
Txoj kev: kuaj pom los ntawm electrospray ionization (esi) ion hom, molecular ion ion ion peak (m +} 1 ([m + h] ⁺).
Txheem: Paub meej qhov tseeb ntawm molecular hnyav, thiab tsis xws luag cuam tshuam los ntawm cov txheej txheem analoguence .
Daim Ntawv Thov: Siv los ua kom meej meej molecular hnyav pov thawj hauv cov qauv ua tiav (xws li cov qauv muaj stabilizers muaj stabilizers) .
Kev Kuaj Xyuas Kev Ruaj Ntseg
Kev Ntsuam Xyuas Kev Ntsuas Ruaj Ntseg
Tej yam kev mob: qhov chaw ntawm 40℃/ 75% RH (txheeb ze rh (txheeb ze cov av noo) rau kev kuaj mob tsis tu ncua {}}
Txheem: Cov ntsiab lus txo qis dua lossis sib npaug rau 10%, impulities tsawg dua los yog sib npaug ntawm 1 {{{2% yog tias kev hloov kho ntawm stabilizers).
Daim Ntawv Thov: twv tau ntev lub sij hawm ntev ruaj ntawm cov khoom ntawm chav tsev ntawm chav tsev, thiab coj kev teeb tsa lub neej txee {}}
Kev Ntsuam Xyuas Kev Ruaj Ntseg
Cov Zwj: Siv Ultrasonicolet Lub Teeb (UV-A / B) rau Irradiate cov qauv los simulate lub teeb ib puag ncig.
Txheem: Cov ntsiab lus txo qis dua lossis sib npaug ntawm 5%, kev siv hluav taws xob tsawg dua lossis muaj kev sib luag rau 0}
Daim Ntawv Thov: Xyuas kom meej tias cov khoom tsis cuam tshuam los ntawm lub teeb thaum kev thauj mus los lossis cia .
Cov Kws Koom Tes Tswj
Cov kuab tshuaj nyob sab
Txoj kev: Ntes Cov Hnyav (xws li DMOPS, Peg400) cov seem los ntawm cov roj chromatography (GC).
Tus Qauv: DMOs residue tsawg dua los yog sib npaug 0 {{{{}} 1%, Peg400 seem tsis muaj tsawg dua lossis sib npaug} 5%. Yog tias qhov seem tau tshaj tus qauv, ua kom cov txheej txheem lim tshuaj (xws li kem chromatography lossis recrystallization).
Daim Ntawv Thov: Zam qhov kev cuam tshuam ntawm cov kuab tshuaj ntawm kev ua ubiological biological lossis kev pheej hmoo txaus ntshai {}}
Cov hlau hnyav thiab cov kev ntsuas microbial
Cov hlau hnyav: Siv cov phiaj xwm ntshav roj av loj (ICP-ms) los xyuas cov hmoov txhuas uas yog txhuas (xws li)
Cov kab mob me: Raws li 2020 Suav Cov Tshuaj, tag nrho cov kab mob suav <100 CLU / ML, ML, ML, ML .
Daim Ntawv Thov: Xyuas kom meej tias cov khoom lag luam ua tau raws cov qauv kev nyab xeeb thiab zam kev kis mob lossis tshuaj lom kev pheej hmoo {}}
Cov Txheej Txheem Txheej Txheem
Nuclear Sib Nqus Revelance (NMR)
Txoj kev: Tshawb cov xeeb ntxwv peaks los ntawm ¹h NMR (400 MHz, DMOPS-D₆) .
Txheem: δ 8 {{{. 52 (s, cyanide-nyob ib sab proton), 4.21 (m, 1h, hydroxyl-propyl proton). Yog hais tias lub ncov txoj hauj lwm lossis tus nqi tseem ceeb yog qhov txawv txav, rov ua hluavtaws lossis kev ua kom huv si yuav tsum muaj.
Daim Ntawv Thov: Paub meej txog kev ncaj ncees ntawm cov qauv molecular, thiab cais cov isomers lossis cov khoom depadation .
Batchquency tswj
Kev Pom Zoo Nruab Nrab
Txoj Kev: Ua kev coj tus cwj pwm tseem ceeb ntawm cov tseem ceeb (xws li sib txuas 9, 10) hauv cov txheej txheem synthesis.
Txheem: Nruab nrab kev coj dawb huv ntau dua los yog sib npaug rau 95%, ua kom muaj kev ruaj ntseg ntawm cov khoom kawg ntawm cov khoom kawg {}}
Daim Ntawv Thov: Txo cov khoom sib txawv-rau-batch los ntawm cov txheej txheem tswj {}}
Ntau tshaj qhia kev soj ntsuam
Txoj kev: coj cov qauv ntawm txhua cov khoom lag luam rau kev rov ua haujlwm ib txwm (xws li kev ntsuas kev coj noj coj ua ib zaug txhua 6 lub hlis).
Txheem: cov khoom uas tau hais kom ua raws cov qauv pib .
Daim ntawv thov: Qaum cov teeb meem zoo thiab tsim kho cov txheej txheem ntau lawm .
Cim npe nrov: Testolone (Rad140 Ua kua), lwm tus neeg, chaw tsim tshuaj paus, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag