text: Ka mea hoʻopuka a MAGL a me ka mea hoʻopuka FAAH: JW-642 & OL-135 & PF-750 ❑ AUSRAw
  /Blog/Gallery/Ka mea hoʻopuka a MAGL a me ka mea hoʻopuka FAAH: JW-642 & OL-135 & PF-750
  Posted on 08 / 15 / 2018 by ʻO Kauka Patrick Young kākauʻo ia i loko Gallery.
  2.Biological Hana-CAS: 1416133-89-5
  4.Biological Hana-CAS: 681135-77-3
  6.Biological Hana-CAS: 959151-50-9
  7. Kālepa JZL-184
  8.Biological Hana-CAS: 1101854-58-3
  9.Highly koho i nā mea hoʻokipa o ka monoacylglycerol lipase e halihali i kahi hui kūʻono
  10.Guide e kūʻai i ka mea hoʻouka o JW-642 MAGL i kēlā me kēia lā
  1. Kākoʻoʻo JW-642
  Kākoʻo iā JW-642 (1416133-89-5) he inhibitor monoacylglycerol lipase (MAGL), koho a me IC50 o 7.6, 14 a me 3.7 nM no ka mouse, ka iole a me ke kanaka MAGL, i kēlā me kēia. ʻO nā endocannabinoids pēnei i ka 2-arachidonoyl glycerol (2-AG) a me ka arachidonoyl ethanolamide he lipid olaola e pili ana i loko o nā hanana synaptic e like me ka hoʻonāʻana o nā mea hōʻailona cannabinoid. ʻO ka Monoacylglycerol lipase (MAGL) he serine hydrolase ka mea e mālama ai i ka hydrolysis o 2-AG i ka waichichiic acid a me glycerol, a pēlā e hoʻopau ai i kāna hana ola. He mea hoʻolālā kūponoʻo JW-642 o ka monoacylglycerol lipase (MAGL) e hōʻike ana i nā kumukānāwai IC50 o 7.6, 14, a me 3.7 nM no ka hanaʻana i ka MAGL ma ka mouse, ka rat, a me nā membrane o ka lolo kanaka, eia kekahi .1 JW-642 koho no MAGL, e koi ana i nā kaʻina o ka kiʻekiʻe nui e hōʻemi i ka hana'aleʻaleʻa amide hana (hydrochse activity) (IC50s = 31, 14, a me 20.6 μM no kaʻiole, iole, a me nā membrane loloʻo kanaka).
  ʻO JW-642 KĀNĀ NUI
  Product inoa ʻO JW-642
  Ka helu CAS 1416133-89-5
  haʻilula C21H20F6N2O3
  Palekana Hoʻopukaʻia i DMSO> 10 mM Pūnaewele Kūʻai ma -20 ° C
  Keʻano kino ʻO kahi hopena ma ka methyl acetate
  Ka Honua Paʻa Hoʻohālikelike ka hopena ho'āʻo: moku me ka hau aniani. Ka nui aʻe o ka nui e hiki ai: moku me RT, aiʻole ka blue ice ma ke noiʻana
  Nā'ōlelo kōkua nui No ka loaʻaʻana o kahi haʻahaʻa kiʻekiʻe, e hoʻomahaʻoe i ka pahu i 37 ℃ a lulu i loko o ka ultrasonic bath no kekahi manawa. E hiki ke mālama ponoʻia nāʻenehana i lalo -20 ℃ no kekahi mau mahina.
  2. Hana Hana-CAS: 1416133-89-5
  ʻO JW-642 ka mea hoʻolālā kaha loa o ka lipoa monoacylglycerol (MAGL) e hōʻike ana i nā kumukānāwai IC50 o 7.6, 14, a me 3.7 nM no ka hanaʻana i ka MAGL ma ka mouse, ka iole, a me nā membrane o ke kanaka. IC50: 7.6 / 14 / 3.7 nM (mouse / rat / kanaka MAGL)
  Ka hopena: Hoʻoponopono ka mea hoʻopiʻi MAGLʻo JW-642 no MAGL, e makemake ana i ka nui o nā haʻina kiʻekiʻe e'ākau i ka hana'aleʻaleʻa amide hydrohese (IC50s = 31, 14, a me 20.6 M no ka mouse, ka iole, a me nā membrane lolo kanaka,).
  3. OL-135 Hōʻuluʻulu
  ʻO OL-135 he mea hōʻailona CNS, he mea hoʻokūpaʻa hoʻokiʻekiʻe loa o FAAH. Hōʻikeʻo OL-135 i nā kahakika analgesic i nāʻano holoholona likeʻole me ka hoʻokalakili kaʻa e pili ana me CB1 agonism.FAAH He mea hōʻailona OL-135 e hoʻohaunaele i ka hōʻailona, ​​akāʻaʻole hoʻohuiʻia, no ka hopohopo pili i ka hoʻouluʻana. Hōʻikeʻia kahi hōʻike kūikawā no nā endocannabinoids i loko o ka manawa o ka makaʻu makaʻuʻole i nā hiʻohiʻona.
  ʻO OL-135 KAUNĀ NUI
  Ka helu CAS 681135-77-3
  Keʻano ʻO ka pauma lepo
  Purity > 98% (aiʻole e nānā i ka Palapala Hoʻoholo)
  Ka Honua Paʻa Hāmeʻaʻia ma lalo o ka mahana wela e like me ka mea hanaʻawaʻole. Ua paʻa kēia huahana no nā pule he nui i ka manawa kūʻai a me ka manawa i hoʻohanaʻia ma kaʻOihana.
  pūnaewele Kūlana: Kino, pouli a ma 0 - 4 C no kekahi mau liʻiliʻi (mau lā i nā hebedoma) aiʻole -20 C no ka wā lōʻihi (mau mahina a hiki i nā makahiki).
  Palekana Hoʻopukaʻia i DMSO,ʻaʻole i ka wai
  Shelf Life > Nā makahiki 2 inā mālama ponoʻia
  Hoʻoponopono waikino Hiki ke hoʻohanaʻia kēia lāʻau lapaʻau ma DMSO
  Kūʻai Storage Storage 0 - 4 C no kekahi manawa pōkole (mau lā i nā wiki), a -20 C no ka wā lōʻihi (mau mahina)
  4. Hana Hana-CAS: 681135-77-3
  ʻO OL-135 he mea hōʻailona CNS, he mea hoʻokūpaʻa hoʻokiʻekiʻe loa o FAAH i loaʻaʻole i ka hana CB1, CB2 a me δ a me nā'ōpipipii opioid e hoʻonui ana i ka hana analgesic a me ka hana hypothermic o ka anandamide.
  ʻO Fatty acid amide hydrolase (FAAH) ka enzyme i kuleana no ka hydrolysis a me ka inactivation o nā amides acetic me ka anandamide a me ka oleamide. PF-750 he mana kūpaʻa, hikiʻole ke hoʻololiʻia, he mea hoʻopiʻiʻole FAAH me nā helu IC50 o 0.6 a me 0.016 μM i ka wā i hoʻomaka muaʻia me FAAH no ka manawa 5 a me 60, e like me kēia .1 Pūnaewele i hanaʻia e like me nā mea pale kanaka a murine. he mea koho nui ka PF-750 no ka FAAH e pili ana i kekahi mau hydrolases serine, me ka hōʻikeʻole i kahi hana pae pūnaewele i hikiʻole iā 500 μM.
  PF-750 NĀ KOINA KUMU
  Product inoa PF-750
  Ka helu CAS 959151-50-9
  Palekana Hoʻopukaʻia ma DMSO
  6. Hana Hana-CAS: 959151-50-9
  PF-750 he mana kūpaʻa, hikiʻole ke hoʻololiʻia e ka FAHA me IC50 waiwai 0.6 a me 0.016 μM i ka wā i hoʻokumu muaʻia me FAAH no ka manawa o 5 a me 60 minuke. ʻO Fatty acid amide hydrolase (FAAH) ka enzyme i kuleana no ka hydrolysis a me ka inactivation o nā amides acetic me ka anandamide a me ka oleamide. Uaʻikeʻia ka hoʻolahaʻana o ka PF-750 i ka mea koho nui no ka FAAH e pili ana i kekahi mau hydrolases serine, me ka hōʻikeʻole i kahi hana pūnaewele hōʻikeʻole i ka 500 μM. Hōʻike ka PF-750 i ka kaha o 10-fold ma mua o URB597 (Sigma # U4133) ma hope o 30 min preincubation. PF-750 nui loa i koho ma FAAH. ʻOiai i like ka nui me 500 μM,ʻaʻohe ona pilina me ka nui o nā enzymes i ho'āʻoʻia, akā,ʻaʻole maikaʻi maikaʻiʻo URB597 a me nā mea hoʻonāukiā'ē aʻe i hoʻomaopopoʻia e ka 100 μM.
  ʻO JZL-184 (1101854-58-3) he mea hoʻokūkū kaha a koho i ka MAGL me IC50 o 8 nM a me 4 μM no ka hanaʻana i ka MAGL a me ka FAAH ma nā pēpi lolo. Ka nui o ka IC50: 8 nM Kekahi: MAHL i loko o ka vitro: JZL-184 ke hoʻolōʻihi nei i ka DSE ma nā pulupulu Purkinje i loko o nā'āpana mele a me DSI ma nā CA1 pyramidal neurons i nā'ōmole hippocampal. ʻO JZL-184 ka meaʻoi loa i ka hanaʻana i ka MAGL maunu ma mua o ka MAGL kānakahi. i loko o vivo: Inā lawelaweʻia e nā mio ma 16 mg / kg, me ka intraperitoneally, JZL-184 ke hoʻohaʻahaʻa i ka MAGL ma o 85%, hoʻonui i ka lolouila 2-AG ma 8-fold, a hoʻolālā i ka hana analgesic ma nāʻanoʻeha o nā maʻi e hoʻohālike pololei hiki i ka cannabinoid central (CB1)'ākena. ʻO ka hoʻoponopono koʻikoʻi o JZL-184 i ka FAAH (- / -) nā mio i hoʻonui i ka nui o nā hāʻina cannabimimetic, hoʻomanaʻo houʻia ka JZL-184 i ka hoʻomanawanui i kona hopena antinociceptive, ka hoʻomanawanui i nā hopena o ka meaʻai o ka Δ-tetrahydrocannabinol, emi iho. i ka 1'-O- (5 - [(3) S] thio) i ka Guanosine 35 - [(XNUMX) S] thio) ka paʻaʻana o triphosphate, a me ka hoʻoikaikaʻana e like me ka hōʻikeʻana i nā halihali hoʻokuʻuʻana i nā rimonabant, me keʻanoʻole o ka genotype.
  JZL -184 NĀ PALAPALA HUI
  Kahi inoa'ē aʻe JZL-184
  haʻilula haʻilula
  kahi KANAKA
  Keʻano ʻO ka'ōmaʻomaʻuʻulaʻula
  Palekana Hoʻopukaʻia ma DMSO (10mg / ml)
  8. Hana Hana-CAS: 1101854-58-3
  Hoʻopā ka JZL-184 i ka MAGL, ka nui o ka enzyme no ka hōʻinoʻana o ka 2-arachidonoylglycerol endocannabinoid (2-AG). ʻO Anandamide a me 2-AG nā endocannabinoids hope loa e hoʻohana nei i nā mea loaʻaʻo CB1 a me CB2 pūnana cannabinoid. ʻO ka nui o ka Anandamide i hoʻokomoʻia e ka fatty acid amide hydrolase (FAAH), akāʻo ka monoacylglycerol lipase (MAGL) ke manaʻoʻiaʻo ka enzyme mua ia no ka hōʻinoʻana o 2-AG. He paʻakikī e hoʻokaʻawale i nā hana a nā meaʻelua no ka meaʻo ka meaʻoi aku o nā mea hana i kēia manawaʻo MAGLʻaʻole i koho, a pāpā hoʻi i ka FAAH a iʻole nā ​​hua'ōlelo'ē aʻe. ʻO JZL-184 ka mea hoʻopiʻi mua i ka MAGL me kaʻoihana nanomolar a ma luna o ka 200-select select for MAGL vs FAAH. I ka lawelaweʻiaʻana e kaʻiole, nui ka piʻiʻana o JZL-184 o ka 2-arachidonoylglycerol ma ka lolo e pili ana i 8-fold, me ka hanaʻole i nā kūlana o ka anandamide.
  9. ʻO nā mea hōʻoki kūpono o ka monoacylglycerol lipase e halihali ana i kahi hui kūʻono
  2-arachidonoyl glycerol (2-AG) a me N-arachidonoyl ethanolamine (anandamide) ka mea i hoʻonāukiukiʻia e ka monoacylglycerol lipase (MAGL) a me ka'alele momona amide hydrolase (FAAH), ma kēlā me kēia. ʻO kaʻike houʻana oʻO-aryl carbamates e like me JZL-184 i koho i nā mea hoʻonāuki MAGL ua hoʻonā i kaʻike pono o nā alanana hōʻailona 2-AG i loko o ka ola. Eia naʻe,ʻo JZL-184 a me nā mea hoʻonāukiʻia MAGL'ē aʻe i hōʻike i keʻano o ka hoʻohālikeʻenehana haʻahaʻa me ka FAAH a me nā transboxral carboxylese, a hiki ke hoʻopili i ko lākou hoʻohanaʻana i kekahi o nā haʻawina ola. Maanei, hōʻike mākou i kahi hui kūikawā o kaʻO-hexafluoroisopropyl (HFIP) carbamates ka mea e hoʻoneʻe ai i MAGL i loko o ka vitro a i loko o ka ola me kaʻoihana maikaʻi a hoʻonui i ka kohoʻana, me ka hōʻikeʻanaʻole i keʻano o ka hawewe-e like me ka FAAH. ʻO kēia mau hopena e hōʻike ana i ka HFIP carbamates ma keʻano he kānana nui no ka hanaʻana i ka MAGL a pono e hoʻoikaika i ka huliʻana i nā mea hana'ē aʻe o nā mea hoʻoheheʻeʻia serine hydrolase e halihali ana i nā hui likeʻole e like me nā hanana o nā pani.
  10. E alakaʻi i ka kūʻaiʻana i ka mea hoʻopuka kūʻaiʻo JW-642 MAGL i kēlā me kēia lā
  ♦ E huli i ka JW-642 Powder (1416133-89-5) ma luna o AASraw
  ♦ Eʻike ʻO JW-642 Powder Windows XP, a kākau i kāu mau koi.
  8 Nā mea koʻikoʻi o ka Powen Stenbolone	ʻO ka 8 ka nui loa o ka hoʻohanaʻana i ka huhū lapaʻau ma ka honua