GS 441524 ， ({{1}} R, {{2}} R, 4 S, {{{4}} R) - { {1}} - (4 - aminopyrrolo [1, {1}, - f] [1, {{1|}}, 4] triazin-7-yl) - {{2}},, 4 - dihydroxy - {{4}} - (hydroxymethyl) tetrahydrofuran- { {1}} - carbonitrile CAS 1 1 9 1 {{{7 {}}}} {{2}} 7-69-0 Kev Qhia

Khoom Piav Qhia

Cov Khoom Muag Khoom: GS 441524 ， ({{1}} R, {{2}} R, 4 S, {{4}} R ) - {{1}} - (4 - aminopyrrolo [1, {{{7 {}}, - f] [1, {{{ 7}}}},, 4] triazin-7-yl) - {{2}},, 4 - dihydroxy - {{4}} - (hydroxymethyl) tetrahydrofuran - {{1}} - carbonitrile CAS 1 1 9 1 {{1}} {7 2}} 7- 69-0

Txhais:

Rov qab ua ntu nrab;

GS-441524;

Tshuaj& Lub cev nqaij daim tawv

Zog: cov hmoov dawb-dawb.

Ntsuas: ≥ 99%

Ntu: 1. 84 ± 0. 1 g

Dej Solubility: Soluble hauv DMSO

Kev piav qhiaS GS-441524 tuaj yeem txwv tsis pub feline kis tus kab mob peritonitis (FIPV), nrog rau EC 50 ntawm 0. 78 μM.

Phiajzeb：

EC 50: 0. 78 μM (FIPV) [1].

Hauv Vitro：

Lub hlwb tshwm sim thiab loj hlob ib txwm muaj ntawm txhua qhov kev sib nkag siab ntawm GS-44 1 524 thiab tsis ua raws li cov xim fluorescent zas CellTox Green ntawm {{1}} h. Cov kua cytotoxic - 50% (CC 50) yog vim li no> 100 μM. Kev ua tau zoo - 50% (EC 50) ntawm GS-44 1 524 tau muab suav rau 0. 78 μM [{1].

Hauv Vivo：

Txhua 10 miv uas kho tau muaj cov lus teb sai rau kev kho thiab qib lymphocyte thiab qhov kub ntawm lub qhov quav rov qab mus rau kev tiv thaiv ua ntej thiab cov theem ntawm ob lub qhov ncauj miv. Ob ntawm 10 kho miv, 1 6 - 1 1 6 (Pawg A) thiab 1 6 - 1 27 (Pawg B ), muaj mob rov ua dua ntawm plaub thiab rau lub lis piam tom qab kev kho mob. Ob tug miv no tau kho ob zaug rau ob lub lim tiam thiab lawv cov lus teb zoo ib yam li thawj txoj kev kho. Tag nrho kaum tus miv ib zaug lossis ob zaug tau rov qab zoo li qub dua li (ntau tshaj li yim lub hlis tom qab kis tau tus mob). Kev txhaj tshuaj ua rau" hloov mus ntxiv; stinging" cov tshuaj tiv thaiv nyob rau hauv qee cov miv hauv 10 s ntawm kev tswj hwm ntawm cov tub ntxhais. Kev mob hauv zos thiab qhov mob ib txwm muaj pov thawj los ntawm kev coj txawv txawv, yaim ntawm qhov chaw txhaj tshuaj thiab / lossis lub suab nrov uas ntev li 30-60 s tom qab txhaj. Kev txhaj tshuaj tiv thaiv kab mob muaj tseeb dua nyob rau qee cov tsiaj txheeb ze rau lwm tus thiab cov kev tawm tsam tsis sib thooj los ntawm ib qho kev txhaj tshuaj rau qhov txuas ntxiv thiab kom tsawg zuj zus ntxiv thaum [1].

Cell Ntsuas：

Txhawm rau txiav txim seb qhov muaj kuab lom ntawm GS-44 1 524 rau CRFK hlwb n, CRFK cov hlwb raug kho nrog {{1,}, 33. 3, {{4} . 1, 3. 7 lossis 1. 2 μM GS-44 1 524 rau {{1 { {12}}}} h [1].

Tsoom thawj coj tsiaj：

Cov miv 2 mg / kg (Pawg B; n=5) GS-44 1 5 24 SC q 24 h pib peb hnub tom qab cov lus tsis txaus ntseeg ntawm FIP (hnub 1 2 - 1 9 kis kab mob). Ob tus miv uas tsis tsim muaj cov cim kab mob ua lub luag haujlwm rau cov ntshav lymphocyte li qub thiab ntsuas kub ntawm lub qhov ncauj [1].

Ua tim khawv：

[1]. Murphy BG, li al. Lub nucleoside analog GS-44 1 524 txwv tsis pub feline kis tus kab mob peritonitis (FIP) kab mob hauv cov nqaij mos thiab kev sim tshuaj miv. Vet Microbiol. 20 1 8 Jun; 2 1 9: 226-233.

GS-441524 yog dab tsi?

Gs-44 1 524 yog qhov tshuaj tiv thaiv tshuaj thib ob tom qab gc {{{1}} ntawm kev kho mob ntawm feline kis peritonitis (FIP). Gs-44 1 524 yog ib qho me me nucleotide analogue uas muab los ntawm Gilead Sciences (Ntiaj teb antiviral teb No. 1) rau perdersencjiaoshou 2 thiab nws cov kev tshawb fawb lub ntsiab lus ntawm kev xa xov hauv plab. Gs-44 1 524 yog ib qho hloov pauv ntawm qhov hloov pauv uas tuaj yeem tiv thaiv qhov tshwm sim ntawm cov feline ntawm lub plab xa mus kis tus kab mob (FIP), thiab ib qho kev ntsuas ua ntej rau kev sib txuas ntawm nucleoside triphosphate nrog cov haujlwm pharmacological. Gs-44 1 524 yog ib qho tshuaj me me, tseem hu ua nucleoside triphosphate sib tw inhibitor, uas muaj cov dej ua kom muaj zog tiv thaiv ntau yam kab mob RNA. Nws tuaj yeem tiv thaiv qhov kev rov ua ntawm ob peb hom kev sib txawv ntawm cov tshuaj lom neeg phau ntawv RNA, xws li mob hnyav ua pa ntawm tus kabmob (SARS), tus kabmob ua pa nruab nrab sab hnub tuaj, tus kab mob Ebola, Lassa ua npaws, tus kab mob Junin thiab tus kab mob ua pa, thiab muaj cytotoxicity tsawg nyob rau hauv cov kab ntawm cov xovtooj ntau.

Lub tshuab ntawm kev ua yog tias GS-441524 yog phosphorylated rau hauv nucleoside monophosphate (NMP) los ntawm cell kinase, thiab tom qab ntawd hloov mus ua peb lub phosphate metabolite (NTP qauv analogue). Hauv viral RNA synthesis, cov nquag NTP txheej txheem ua haujlwm ua haujlwm ua raws li kev sib tw ntawm ntuj nucleoside triphosphate thiab kev sib tw ntawm ntuj nucleoside (ATP, TTP, CTP, GTP) kom koom nrog hauv RNA transmissions. Thaum gs-441524 tau muab tso rau hauv cov khoom xa tawm, cov khoom xa tawm yuav raug txiav ua ntej, yog li thaiv cov txheej txheem kis kab mob RNA.

Yog tias koj txaus siab rau peb cov khoom lossis muaj lus nug, thov koj xav tiv tauj peb!

Cov khoom lag luam hauv qab patent yog muab rau R& D lub hom phiaj nkaus xwb. Txawm li cas los xij, lub luag haujlwm kawg tau txiav txim siab nrog cov neeg yuav khoom.

Cim npe nrov: gs 441524 ， ({{1}} r, {{2}} r, {4 s, {{4}} r) - { {1}} - (4 - aminopyrrolo [1, {1}, - f] [1, {{1|}}, 4] triazin-7-yl) - {{2}},, 4 - dihydroxy - {{4}} - (hydroxymethyl) tetrahydrofuran- { {1}} - carbonitrile cas 1 1 9 1 {1}} {{2}} 7-69-0 , tuam ntxhab, cov chaw muag khoom, lub Hoobkas, yuav, hauv Tshuag

• Tug: D-Altrononitrile, {{4}} - C - (4 - aminopyrrolo [{4,}, 1 - f] [1, {{4},, 4] triazin-7-yl) - {{{{8 8}}}, 5-anhydro-3, 4 - O - ({{ 6}} - methylethylidene) CAS 1 1 9 1 {{4}} 37-80-5
• Tom ntej: (3 R, {{1}} R, {{2} R) - 2 - ({{1}} - aminopyrrolo [ 2, 1 - f] [1, 2, {{1,] {triazin-7-yl) - 3, {{1}} - bis (benzyloxy) - {{2}} - ((benzyloxy) methyl) tetrahydrofuran - 2 - ol CAS 1 {{0 } {{{{5 {}}}} {{{5 {}}}} 0 {1}} 9-9 {{1}} - 3 |