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Uhlolo lwe-1.JW-642
Umsebenzi we-2.Biological-CAS: 1416133-89-5
Uhlolo lwe-3.OL-135
Umsebenzi we-4.Biological-CAS: 681135-77-3
5. Uvavanyo lwe-PF-750
Umsebenzi we-6.Biological-CAS: 959151-50-9
7. Ukuhlaziywa kwe-JZL-184
Umsebenzi we-8.Biological-CAS: 1101854-58-3
I-9.Inhibitors ekhethayo ye-monoacylglycerol lipase ethwele iqela elisebenzayo
10.Guide ukuthenga i-JW-642 MAGL inhibitor inyathelo ngesinyathelo


Ividiyo yeJW 642


I.JW 642 Abalinganiswa basisiseko:

igama: JW 642
CAS: 1416133-89-5
I-molecular Formula: C21H20F6N2O3
Isisindo somzimba: 462.4
Melt Point:
Isitoreji sokugcina: kwi -20 ° C iminyaka eyi-3 Ubuninzi
umbala: OMhlophe


1. Ukuhlaziywa kwe-JW-642aasraw

JW-642 (1416133-89-5) i-monoacylglycerol lipase (MAGL) ye-inhibitor ene-IC50 ye-7.6, i-14 kunye ne-3.7 nM ye-mouse, i-rat kunye ne-MAGL yabantu ngokulandelanayo. I-Endocannabinoids efana ne-2-arachidonoyl glycerol (i-2-AG) kunye ne-arachidonoyl ethanolamide ziyi-lipids ezisebenzayo ezibandakanyekayo kwiinkqubo ezili-synaptic ezibandakanya ukuphunyezwa kwee-receptors ze-cannabinoid. I-Monoacylglycerol lipase (MAGL) yi-serine hydrolase ejongene ne-hydrolysis ye-2-AG i-arachidonic acid kunye ne-glycerol, ngaloo ndlela iphelisa umsebenzi wayo. I-JW-642 inhibitor enamandla ye-monoacylglycerol lipase (MAGL) ebonisa ii-IC50 iimpawu ze-7.6, i-14, kunye ne-3.7 nM yokuvinjelwa kwe-MAGL kwi-mouse, i-rat, kunye ne-brain membranes, ngokulandelanayo .1 JW-642 ikhetha i-MAGL, ukufuna iindawo eziphezulu kakhulu ukwenzela ukuvimbela ngokusemthethweni umsebenzi we-acid amide hydrolase (IC50s = 31, 14, kunye ne-20.6 μM nge mouse, i-rat, kunye ne-brain membranes) ngokulandelanayo).

I-JW-642 IINKCUKACHA ZEZIKHONO
Igama lemveliso JW-642
Inombolo yeCAS 1416133-89-5
formula C21H20F6N2O3
M.Wt 462.39
Umzimba I-DMSO> I-10 mM Isitoreji seSitoreji kwi -20 ° C
Imbonakalo yomzimba Isisombululo kwi-methyl acetate
Imiqathango Yokuthumela Isampula yokuhlola isampula: iinqanawa nge-blue ice.Wonke ubukhulu obukhoyo: umkhumbi kunye ne-RT, okanye iqhwa elihlaza okwesibhakabhaka xa kuceliwe
Iingcebiso jikelele Ukuze ufumane ubunqamle obuphezulu, nceda ushuthule ityhubhu kwi-37 ℃ kwaye uyigubungele kwibhanki ye-ultrasonic kwithuba elithile. Isisombululo sendawo singagcinwa ngezantsi -20 ℃ ngeenyanga eziliqela.



I-Raw JW 642 powder (1416133-89-5) hplc =98% | I-powder powder


2. Umsebenzi we-Biological-CAS: 1416133-89-5aasraw

I-JW-642 inhibitor enamandla ye-monoacylglycerol lipase (MAGL) ebonisa ixabiso le-IC50 ye-7.6, i-14, kunye ne-3.7 nM yokuvimbela i-MAGL kwi-mouse, i-rat, kunye ne-membrane yengqondo, ngokulandelanayo. IC50: 7.6 / 14 / 3.7 nM (imouse / i-rat / i-MAGL yabantu)
Ithagethi: i-MAGL inhibitor i-JW-642 ikhetha i-MAGL, idinga ukufikelela kwiindawo eziphezulu kakhulu ukwenzela ukuvimbela ngokuthe tye umsebenzi we-fatty acid amide hydrolase (IC50s = 31, 14, kunye ne-20.6 M ye mouse, i-rat, kunye ne-brain membranes).


3. Uhlolo lwe-OL-135aasraw

OL-135 ngu-CNS owangena, onamandla kakhulu kwaye okhethiweyo ongenayo i-FAAH. I-OL-135 ibonisa i-analgesic pharmacology kwiimpawu ezahlukeneyo zezilwanyana ngaphandle kokuphazamiseka kweemoto ezinxulumene ne-CB1 agonism ngqo.AAH Inhibitor OL-135 iphazamisa ukufumana, kodwa ingahlanganisi, ukuxhomekeka kwimeko yokutya. Ukumelana nokutya nokuxhatshazwa kwe-reactivity kuyaqhubeka kungathinteki. Idata ibonisa indima ethile kwi-endocannabinoids kwisigcawu sokwesaba imeko yama-paradigms.

I-OL-135 IINKCUKACHA ZEZIKHONO
Igama lemveliso OL-135
Inombolo yeCAS 681135-77-3
Kubonakala Powder
Ukungcola > 98% (okanye ubhekisele kwiSatifikethi soHlololo)
Imiqathango Yokuthumela Ukuthunyelwa phantsi kobushushu obumgangatho obuninzi njengemichiza engabungozi. Lo mveliso uzinzile ngokwaneleyo kwiiveki ezimbalwa ngexesha lokuthumela ngokuqhelekileyo kunye nexesha elichithwe kwiDavi.
yoGcino Imeko Emile, emnyama kunye ne-0 - 4 C ngexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (inyanga ukuya kwiminyaka).
Umzimba Isisombululo kwi-DMSO, kungekhona emanzini
Beka ubomi kwishelufa > Iminyaka ye-2 ukuba igcinwe kakuhle
UkuPhathwa kweziMilo Esi sidakamizwa sinokuqulunqwa kwi-DMSO
Isitoreji seStock Solution 0 - 4 C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20 C ixesha elide (iinyanga)


4. Umsebenzi we-Biological-CAS: 681135-77-3aasraw

OL-135 ngu-CNS owangena, onamandla kakhulu kwaye okhethiweyo oguqulwayo we-FAAH ongenayo i-CB1, i-CB2 kunye ne-δ imisebenzi ye-opioid receptors eyenza umsebenzi we-anandamide wenziwe nge-analgesic ne-hypothermic.


5. Uvavanyo lwe-PF-750aasraw

I-fatty acid amide hydrolase (FAAH) yi-enzyme ejongene ne-hydrolysis kunye nokungasebenzi kwe-acid acid amides kuquka i-anandamide ne-oleamide. PF-750 inamandla, ixhomekeka ngexesha, i-FAAH inhibitor engenakuphikiswa kunye ne-IC50 ixabiso le-0.6 kunye ne-0.016 μM xa i-FAAH ibuyele i-FAAH emfutshane ngemizuzu eyi-5 kunye ne-60 ngokulandelanayo. I-PF-1 ikhethe kakhulu i-FAAH malunga namanye ama-serine hydrolases, engabonakali nento engacacisiyo yomsebenzi ukuya kwi-750 μM.

PF-I750 IINKCUKACHA ZEZIKHONO
Igama lemveliso PF-750
Inombolo yeCAS 959151-50-9
Kubonakala Powder
Ukungcola > 98% (okanye ubhekisele kwiSatifikethi soHlololo)
Imiqathango Yokuthumela Ukuthunyelwa phantsi kobushushu obumgangatho obuninzi njengemichiza engabungozi. Lo mveliso uzinzile ngokwaneleyo kwiiveki ezimbalwa ngexesha lokuthumela ngokuqhelekileyo kunye nexesha elichithwe kwiDavi.
yoGcino Imeko Emile, emnyama kunye ne-0 - 4 C ngexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (inyanga ukuya kwiminyaka).
Umzimba Isisombululo kwiDMSO
Beka ubomi kwishelufa > Iminyaka ye-2 ukuba igcinwe kakuhle
UkuPhathwa kweziMilo Esi sidakamizwa sinokuqulunqwa kwi-DMSO
Isitoreji seStock Solution 0 - 4 C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20 C ixesha elide (iinyanga)


6. Umsebenzi we-Biological-CAS: 959151-50-9aasraw

PF-750 inamandla, ixhomekeka ngexesha, i-FAAH inhibitor engenakuphikiswa kunye ne-IC50 neempawu ze-0.6 kunye ne-0.016 μM xa i-FAAH ibuye ixhaswe nge-5 kunye ne-60 imizuzu ngokulandelanayo. I-fatty acid amide hydrolase (FAAH) yi-enzyme ejongene ne-hydrolysis kunye nokungasebenzi kwe-acid acid amides kuquka i-anandamide ne-oleamide. Isalathisi esekelwe kwimisebenzi yeesampuli ze-proteome ezihlukeneyo zomntu kunye nezidumbu zibonisa ukuba i-PF-750 ikhetha i-FAAH ngokumalunga namanye ama-serine hydrolases, engabonakali nento engaqondakaliyo ngaphandle kwe-500 μM. PF-750 ibonisa i-10 ngeyona ndlela engcono kune-URB597 (Sigma # U4133) emva kwe-30 min yangaphambili. PF-750 ikhethe kakhulu kwi-FAAH. Kwanokuphakama nje nge-500 μM, kwakungekho nxu lumano kunye ne-enzymes ezininzi ezivivinywe, kodwa i-URB597 kunye namanye ama-FAAH inhibitors awayaziwayo ayenzi kakuhle kwi-concentrating ephantsi (100 μM).

MAGL inhibitor kunye ne-FAAH Inhibitor JW-642 & OL-135 & PF-750


7. Ukuhlaziywa kwe-JZL-184aasraw

I-JZL-184 (1101854-58-3) i-inhibitor enamandla kwaye ekhethiweyo ye-MAGL kunye ne-IC50 ye-8 nM kunye ne-4 μM ukwenzela ukuvinjelwa kwe-MAGL ne-FAAH kwimimbrane yobuchopho. Ixabiso le-IC50: I-8 nM I-Target: i-MAGL inhibitor kwi-vitro: I-JZL-184 ilandisa i-DSE kwi-Purkinje neurons kwiimpawu ze-cerebellar kunye ne-DSI kwi-CA1 i-pyramidal neurons kwimigqomo ye-hippocampal. I-JZL-184 inamandla kakhulu ekuvimbeleni i-mouse MAGL kune-rat MAGL. kwi-vivo: Xa ilawulwa kwiigundane kwi-16 mg / kg, i-intraperitoneally, i-JZL-184 iyanciphisa umsebenzi we-MAGL ngu-85%, iphakamisa amaqondo e-2-AG ngengqondo nge-8, kwaye yenza umsebenzi ohlotshaniswayo kwiimvavanyo zeentlungu ezinokulinganisa ophakathi kwe-cannabinoid (CB1). Ukulawulwa kakuhle kwe-JZL-184 ku-FAAH (- / -) iigundlo eziphucukisiwe ubukhulu be-subset yeempendulo ze-cannabimmetic, unyango oluphindaphindiweyo lwe-JZL-184 lukhokelela ekunyamezelaneni nemiphumo ye-antinociceptive, ukunyamezelana kwemiphumo ye-pharmacological ye-Δ-tetrahydrocannabinol, kunciphisa kwi-CB1 i-receptor receptor-ivuselele i-guanosine i-5'-O- (3 - [(35) S] thio) i-triphosphate ebophayo, kunye nokuxhomekeka njengoko kuboniswa ziziphathamandla zokurhoxiswa kwe-irmonabant-precipitated, kungakhathaliseki i-genotype.

JZL -184 IINKCUKACHA ZEZIKHONO
Igama elongezelelweyo JZL-184
formula formula
MW 520.5
imvelaphi AASraw
CAS 1101854-58-3
Ukungcola ≥98% (TLC)
Kubonakala Uluhlaza obomvu
Umzimba I-Soluble kwi-DMSO (10mg / ml)


8. Umsebenzi we-Biological-CAS: 1101854-58-3aasraw

I-JZL-184 inqanda i-MAGL, i-enzyme eyona nto ijongene nokuthotywa kwe-endocannabinoid 2-arachidonoylglycerol (2-AG). I-Anandamide kunye ne-2-AG ziyi-endocannabinoids ezinokuphela ezinokuthi zenze i-receptors ye-cannabinoid CB1 ne-CB2. I-Anandamide ixhaswa kakhulu ngamafutha ase-acide hydrolase (FAAH), kanti i-monoacylglycerol lipase (i-MAGL) icingelwa ukuba yi-enzyme eyona nto ibangela uxanduva lwe-2-AG. Kunzima ukwahlula imisebenzi yezo zibini kuba ezininzi ezikhoyo ezikhoyo kwi-MAGL azikhethi, kwaye zivimbela i-FAAH okanye ezinye i-enzymes. I-JZL-184 iyona yeyokuqala inhibitor yokukhetha ye-MAGL kunye ne-nanomolar portency kunye no-200-fold selectivity for MAGL vs FAAH. Xa ilawulwa kwiigundane, i-JZL-184 yanda amazinga e-2-arachidonoylglycerol ebuchosheni malunga ne-8, ngokungekho miphumo kumanqanaba e-anamamide.


9. I-inhibitors ephezulu ye-monoacylglycerol lipase ethwele iqela elisebenzayoaasraw



I-endocannabinoids i-2-arachidonoyl glycerol (i-2-AG) kunye ne-N-arachidonoyl ethanolamine (i-anamamide) ihlaziywa kakhulu yi-monoacylglycerol lipase (MAGL) kunye ne-fatty acid amide hydrolase (FAAH), ngokulandelanayo. Ukufunyanwa kwangoko kwe-O-aryl carbamates efana ne-JZL-184 njengendlela yokukhetha i-MAGL inhibitors iye yakwenza uphando olusebenzayo lwe-2-AG indlela yokutshintshela kwi-vivo. Nangona kunjalo, i-JZL-184 kunye nezinye i-MAGL inhibitors ezibikwayo zibonakalisa i-low-level reactivity nge-FAAH kunye ne-peripheral carboxylesterases, ezinokuthi zibenzima ukusetyenziswa kwezifundo ezithile. Apha, sichaza iklasi ehlukileyo ye-O-hexafluoroisopropyl (HFIP) carbamates evimbela i-MAGL kwi-vitro kwaye i-vivo ibe nefuthe elihle kakhulu kwaye iphucule kakhulu ukhetho, kubandakanyeka ukubonisa akukho-reactivity ebonakalayo ne-FAAH. Ezi ziphumo zichaza i-HFIP carbamates njenge-chemotype ephathekayo yokuvimbela i-MAGL kwaye kufuneka ikhuthaze ukulandela ezinye i-serine hydrolase inhibitors ezithwala amaqela asebenzayo afana nezakhiwo ze-substrates zendalo.


10. Isikhokelo ekuthengeni i-JW-642 MAGL inhibitor Inyathelo nenyatheloaasraw

♦ I-Google AASraw, faka kwi-www.aasraw.com.
♦ Khangela i-JW-642 Powder (1416133-89-5) kwi-AASraw
♦ Khangela I-JW-642 Powder Windows XP, kwaye ubhale phantsi iifirmnets zakho.
♦ Sifumana i-imeyile yakho kwaye sithetha ezinye iinkcukacha nawe.
♦ Qinisekisa umyalelo, ngoko intlawulo yenziwe kwaye siza kulungiselela iimpahla zokuhambisa emva kwakho.


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