I-MAGL inhibitor kunye ne-FAAH Inhibitor: JW-642 kunye ne-OL-135 kunye ne-PF-750 丨 AASraw
I-AASraw ivelisa i-Cannabidiol (CBD) ipowder kunye ne-Hemp ebalulekileyo yeoyile ngobuninzi!

 

Yonke into ngeMibolerone (Hlola amaconsi)

 

  Uhlolo lwe-1.JW-642
  Umsebenzi we-Biological-CAS: 2-1416133-89
  Uhlolo lwe-3.OL-135
  Umsebenzi we-Biological-CAS: 4-681135-77
  5. Uphengululo lwePF-750
  Umsebenzi we-Biological-CAS: 6-959151-50
  7. Uphengululo lweJZL-184
  Umsebenzi we-Biological-CAS: 8-1101854-58
  I-9.Inhibitors ekhethayo ye-monoacylglycerol lipase ethwele iqela elisebenzayo
  Isikhokelo sokuthenga i-JW-10 MAGL inhibitor inyathelo ngenyathelo

 


 

Ividiyo yeJW 642

 

 


 

I.JW 642 Abalinganiswa basisiseko:

 

igama: JW 642
CAS: 1416133-89-5
Ifomula yeMolekyuli: C21H20F6N2O3
Ubunzima Ezinto: 462.4
Melt Point:
Isitoreji sokugcina: kwi -20 ° C iminyaka eyi-3 Ubuninzi
umbala: OMhlophe

 


 

1. Ukuhlaziywa kwe-JW-642aasraw

 

JW-642 (1416133-89-5Inamandla, ikhetha i-monoacylglycerol lipase (MAGL) inhibitor ene-IC50 ye-7.6, 14 kunye ne-3.7 nM yeempuku, i-rat kunye ne-MAGL yabantu, ngokwahlukeneyo. I-Endocannabinoids ezinje nge-2-arachidonoyl glycerol (2-AG) kunye ne-arachidonoyl ethanolamide zii-lipids ezisebenzayo zebhayoloji ezichaphazelekayo kwiinkqubo ezininzi ze-synaptic kubandakanya ukwamkelwa kwee-cannabinoid receptors. I-Monoacylglycerol lipase (MAGL) yi-serine hydrolase ejongene ne-hydrolysis ye-2-AG ukuya kwi-arachidonic acid kunye ne-glycerol, yiyo loo nto iphelisa ukusebenza kwayo. I-JW-642 sisithinteli esinamandla se-monoacylglycerol lipase (MAGL) esibonisa amaxabiso e-IC50 ye-7.6, 14, kunye ne-3.7 nM yokuthintela i-MAGL kwimouse, iirati, kunye neembrane zengqondo yomntu, ngokulandelanayo. 1 JW-642 ikhetha iMAGL, ifuna ukugxila okuphezulu kakhulu ukuthintela ngokufanelekileyo i-asidi ye-asidi ye-amide hydrolase (ii-IC50s = 31, 14, kunye ne-20.6 µM yeempuku, iirati, kunye neembrane zobuchopho bomntu, ngokulandelelana).

 

I-JW-642 IINKCUKACHA ZEZIKHONO
Igama lemveliso JW-642
Inombolo yeCAS 1416133-89-5
formula C21H20F6N2O3
M.Wt 462.39
Umzimba I-Soluble kwi-DMSO> i-10 mM yokugcina 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 sisithinteli esinamandla se-monoacylglycerol lipase (MAGL) esibonisa amaxabiso e-IC50 ye-7.6, 14, kunye ne-3.7 nM yokuthintela i-MAGL kwimpuku, kumqolo, nakwizinwe zobuchopho bomntu, ngokulandelelana. I-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 bhekisa kwiSatifikethi soHlalutyo)
Imiqathango Yokuthumela Ukuthunyelwa phantsi kobushushu obumgangatho obuninzi njengemichiza engabungozi. Lo mveliso uzinzile ngokwaneleyo kwiiveki ezimbalwa ngexesha lokuthumela ngokuqhelekileyo kunye nexesha elichithwe kwiDavi.
yoGcino Imeko Okomileyo, omnyama kunye no-0 ukuya ku-4 C okwexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).
Umzimba Isisombululo kwi-DMSO, kungekhona emanzini
Beka ubomi kwishelufa > Iminyaka emi-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. Uphengululo lwePF-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 bhekisa kwiSatifikethi soHlalutyo)
Imiqathango Yokuthumela Ukuthunyelwa phantsi kobushushu obumgangatho obuninzi njengemichiza engabungozi. Lo mveliso uzinzile ngokwaneleyo kwiiveki ezimbalwa ngexesha lokuthumela ngokuqhelekileyo kunye nexesha elichithwe kwiDavi.
yoGcino Imeko Okomileyo, omnyama kunye no-0 ukuya ku-4 C okwexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).
Umzimba Isisombululo kwiDMSO
Beka ubomi kwishelufa > Iminyaka emi-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

 

I-PF-750 inamandla, ixhomekeke kwixesha, i-FAAH inhibitor engenakuphikwa ine-IC50 yexabiso le-0.6 kunye ne-0.016 μM xa iphinda yenziwe ngaphambili nge-FAAH yabantu yemizuzu emi-5 kunye nama-60, ngokulandelelana. I-fatty acid amide hydrolase (FAAH) yi-enzyme ejongene ne-hydrolysis kunye nokungasebenzi kwe-acid acid amide kubandakanya i-anandamide kunye ne-oleamide. Umsebenzi osekwe kwiprofayili yovavanyo lweesampulu ezahlukeneyo zomntu kunye nomchamo ziveze ukuba i-PF-750 ikhetheke kakhulu kwi-FAAH xa kuthelekiswa nezinye i-serine hydrolases, ingabonakalisi msebenzi ubonakalayo ngaphandle kwesiza ukuya kuthi ga kwi-500 μM. I-PF-750 ibonisa amandla angama-10 angcono kune-URB597 (Sigma # U4133) emva kwe-30 min preincubation. I-PF-750 ikhetheke kakhulu kwi-FAAH. Nokuba iphakame kangange-500 μM, ibingenalo unxibelelwano nee-enzymes ezininzi ezivavanyiweyo, kodwa i-URB597 kunye nezinye ii-inhibitors ze-FAAH ezingakhange zisebenze kakuhle ekugxininiseni okuphantsi (100 μM).

 

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

 


 

7. Uphengululo lweJZL-184aasraw

 

I-JZL-184 (1101854-58-3) yeyona nto inamandla kunye nokukhetha inhibitor ye-MAGL ene-IC50 ye-8 nM kunye ne-4 μM yokuthintela i-MAGL kunye ne-FAAH kwiimbumba zobuchopho ngokulandelelana. Ixabiso le-IC50: 8 nM Ithagethi: MAGL inhibitor in vitro: I-JZL-184 yongeza i-DSE kwii-Purkinje neurons kwizilayi ze-cerebellar kunye ne-DSI kwi-CA1 i-pyramidal neurons kwizilayi ze-hippocampal. I-JZL-184 inamandla ngakumbi ekuthinteleni i-mouse MAGL kune-rat MAGL. kwi-vivo: Xa ilawulwa kwiimpuku kwi-16 mg / kg, ngaphakathi, i-JZL-184 inciphisa umsebenzi we-MAGL nge-85%, iphakamisa amanqanaba engqondo ye-2-AG nge-8-fold, kwaye inyusa imisebenzi ye-analgesic kwiintlobo ngeentlobo zeentlungu ezilinganisa ngokuthe ngqo ukulinganisa ngqo i-cannabinoid esembindini (CB1) i-agonists. Ulawulo olunamandla lwe-JZL-184 ukuya kwi-FAAH (- / -) iimpuku zonyusa ubungakanani beseti yeempendulo ze-cannabimimetic, unyango oluphindaphindiweyo lwe-JZL-184 lukhokelele kunyamezelo kwiziphumo zalo zokunyanga ukunganyamezeli, ukunyamezelana kwiziphumo ze-ological-tetrahydrocannabinol kwi-CB1 i-receptor agonist-evuselelekileyo i-guanosine 5'-O- (3 - [(35) S] thio) triphosphate yokubopha, kunye nokuxhomekeka njengoko kubonisiwe kukuziphatha okungafunekiyo kwe-rimonabant, ngaphandle kohlobo lwe-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 ikhetha ukuthintela i-MAGL, i-enzyme ikakhulu inoxanduva lokuthotywa kwe-endocannabinoid 2-arachidonoylglycerol (2-AG). I-Anandamide kunye ne-2-AG zii-endocannabinoids ezimbini ezingapheliyo ezenza ii-cannabinoid receptors CB1 kunye ne-CB2. I-Anandamide ubukhulu becala i-acid acid i-amide hydrolase (i-FAAH), ngelixa i-monoacylglycerol lipase (MAGL) kucingelwa ukuba yi-enzyme ikakhulu ejongene nokuthotywa kwe-2-AG. Kunzima ukwahlulahlula imisebenzi yezi zimbini kuba uninzi lwee-inhibitors ezikhoyo ze-MAGL azikhethi, kwaye zithintela i-FAAH okanye ezinye ii-enzymes. I-JZL-184 yeyona inhibitor yokuqala yokukhetha ye-MAGL ene-nanomolar portency kunye nokukhetha okungaphezulu kwama-200 kwi-MAGL vs FAAH. Xa ulawulwa kwiimpuku, i-JZL-184 inyuse amanqanaba e-2-arachidonoylglycerol kwingqondo malunga ne-8-fold, ngaphandle kwesiphumo kumanqanaba e-anandamide.

 


 

9. I-inhibitors ekhetheke kakhulu 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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