MAGL inhibitor ndi FAAH Inhibitor: JW-642 & OL-135 & PF-750 丨 AASraw
AASraw imapanga ufa wa Cannabidiol (CBD) ndi Hemp Mafuta Ofunika ambiri!

 

Chilichonse chokhudza Mibolerone (Fufuzani madontho)

 

  Zotsatira za 1.JW-642
  Ntchito Yachilengedwe - CAS: 2-1416133-89
  Zotsatira za 3.OL-135
  Ntchito Yachilengedwe - CAS: 4-681135-77
  5. Kuwunika kwa PF-750
  Ntchito Yachilengedwe - CAS: 6-959151-50
  7. Kuwunikira kwa JZL-184
  Ntchito Yachilengedwe - CAS: 8-1101854-58
  9.Masewera osankhidwa a monoacylglycerol lipase omwe amachititsa gulu lokhazikika
  10. Onetsetsani kuti mugule JW-642 MAGL inhibitor sitepe ndi sitepe

 


 

JW 642 kanema

 

 


 

I.JW 642 Anthu oyambirira:

 

Name: JW 642
CAS: 1416133-89-5
Maselo chilinganizo: C21H20F6N2O3
Kulemera kwa Maselo: 462.4
Melt Point:
Kusungirako nyengo: pa -XUMUM ° C Zaka 20 Powder
mtundu; White olimba

 


 

1. JW-642 Reviewaasraw

 

JW-642 (1416133-89-5) ndi inhibitor yamphamvu, yosankha monoacylglycerol lipase (MAGL) yokhala ndi IC50 ya 7.6, 14 ndi 3.7 nM ya mbewa, makoswe ndi MAGL a anthu, motsatana. Endocannabinoids monga 2-arachidonoyl glycerol (2-AG) ndi arachidonoyl ethanolamide ndi lipids yogwira ntchito yomwe imakhudzidwa ndimachitidwe angapo a synaptic kuphatikiza kuyambitsa ma cannabinoid receptors. Monoacylglycerol lipase (MAGL) ndi serine hydrolase yomwe imayambitsa hydrolysis ya 2-AG kupita ku arachidonic acid ndi glycerol, motero kumathetsa ntchito yake yachilengedwe. JW-642 ndi inhibitor yamphamvu ya monoacylglycerol lipase (MAGL) yomwe imawonetsera IC50 mitengo ya 7.6, 14, ndi 3.7 nM yoletsa MAGL mu mbewa, makoswe, ndi ma membranes amunthu, motsatana. 1 JW-642 imasankha MAGL, zomwe zimafunikira kuchuluka kwambiri kuti zilepheretse mafuta acid amide hydrolase zochita (IC50s = 31, 14, ndi 20.6 µM ya mbewa, makoswe, ndi mamina am'magazi, motsatana).

 

JW-642 ZOKHUDZA ZOTHANDIZA
dzina mankhwala JW-642
Nambala ya CAS 1416133-89-5
chilinganizo C21H20F6N2O3
M.Wt 462.39
Kutupa Kusungunuka mu DMSO> 10mM Store Store pa -20 ° C
Kuwoneka Kwawo Yankho mu methyl acetate
Kutumiza Chikhalidwe Kufufuza njira yothetsera: kutumiza ndi ayezi wonyezimira.Zowonjezera zina zonse: ngalawa ndi RT, kapena ayezi a buluu pa pempho
Mfundo zambiri Kuti mupeze kutentha kwapadera, chonde muziwotcha chubu pa 37 ℃ ndikugwedezani mu akusamba kwa kanthawi. Njira yothetsera imatha kusungidwa pansipa -20 ℃ kwa miyezi ingapo.

 

Mphungu JW 642 ufa (1416133-89-5) hplc≥98% | Nkhosa yowonjezera

 


 

2. Ntchito Yachilengedwe - CAS: 1416133-89-5aasraw

 

JW-642 ndi inhibitor yamphamvu ya monoacylglycerol lipase (MAGL) yomwe imawonetsera IC50 mitengo ya 7.6, 14, ndi 3.7 nM yoletsa MAGL mu mbewa, makoswe, ndi ma membranes amunthu, motsatana. IC50: 7.6 / 14 / 3.7 nM (mbewa / makoswe / MAGL aanthu)
Zolinga: MAGL inhibitor JW-642 imasankha MAGL, yomwe imakhala ndi malo okwera kwambiri kuti iwonetsetse mafuta a acid amide hydrolase (IC50s = 31, 14, ndi 20.6 M chifukwa cha mbewa, makoswe, ndi ubongo waumunthu).

 


 

3. OL-135 Reviewaasraw

 

OL-135 ndi CNS wodaliritsa, wolimba kwambiri komanso wosasinthika wotsutsana ndi FAAH. OL-135 ikuwonetsa analgesic pharmacology mu zitsanzo zamtundu wanyama popanda zofooka zamagalimoto zomwe zimagwiridwa mwachindunji CB1 agonism.FAAH Inhibitor OL-135 imasokoneza kugula, koma osati kuphatikizana, ndi chikhalidwe chowopsya chenichenicho.Kuopa mantha ndi kukhumudwa kumakhalabe kosakhudzidwa. Deta imatanthawuza udindo weniweni wa endocannabinoids mu gawo la mantha a paradigms.

 

OL-135 TECHNICAL DATA
Name mankhwala OL-135
Nambala ya CAS 681135-77-3
Maonekedwe Mpweya wolimba
Chiyeretso > 98% (kapena onetsani satifiketi yakusanthula)
Kutumiza Chikhalidwe Kutumizidwa pansi pa kutentha monga mankhwala osakhala oopsa. Chogulitsa chimenechi n'chokhazikika kwa masabata angapo panthawi yamtundu wamba komanso nthawi yomwe amatha ku Customs.
Ulili yosungirako Youma, mdima ndi 0 - 4 C kwakanthawi kochepa (masiku mpaka masabata) kapena -20 C kwakanthawi (miyezi mpaka zaka).
Kutupa Kusungunuka mu DMSO, osati m'madzi
Phalala > Zaka ziwiri ngati zasungidwa bwino
Kupanga Mankhwala Mankhwalawa angapangidwe mu DMSO
Stock Solution yosungirako 0 - 4 C kwakanthawi kochepa (masiku mpaka masabata), kapena -20 C kwakanthawi (miyezi)

 

 


 

4. Ntchito Yachilengedwe - CAS: 681135-77-3aasraw

 

OL-135 ndi CNS yomwe imalowa, yomwe imakhala yolimba kwambiri komanso yosasinthika ya FAAH yomwe ilibe CB1, CB2 ndi μ ndi δ opioid receptors ntchito zomwe zimapangitsa ntchito ya analandic ndi hypothermic ya anandamide.

 


 

5. Kuwunika kwa PF-750aasraw

 

Fatty acid amide hydrolase (FAAH) ndiyo nyamayi yomwe imayambitsa hydrolysis ndi kusokoneza mafuta amchere amide kuphatikizapo anandamide ndi oleamide. PF-750 ndi yodalirika, yodalira nthawi, yosasinthika FAAH inhibitor yomwe ili ndi IC50 mikhalidwe ya 0.6 ndi 0.016 μM pamene imayambitsidwa ndi FAAH yomwe imapangidwanso kwa 5 ndi 60 maminiti, mowirikiza.1 Ntchito yofotokozera za mitundu yambiri ya anthu ndi minofu ya proteome inavumbulutsidwa kuti PF-750 imasankha kwambiri FAAH ndi zina zotchedwa serine hydrolases, zosonyeza kuti palibe ntchito yodalirika yopita ku 500 μM.

 

PF-750 MFUNDO ZOFUNIKA
dzina mankhwala PF-750
Nambala ya CAS 959151-50-9
Maonekedwe Mpweya wolimba
Chiyeretso > 98% (kapena onetsani satifiketi yakusanthula)
Kutumiza Chikhalidwe Kutumizidwa pansi pa kutentha monga mankhwala osakhala oopsa. Chogulitsa chimenechi n'chokhazikika kwa masabata angapo panthawi yamtundu wamba komanso nthawi yomwe amatha ku Customs.
Ulili yosungirako Youma, mdima ndi 0 - 4 C kwakanthawi kochepa (masiku mpaka masabata) kapena -20 C kwakanthawi (miyezi mpaka zaka).
Kutupa Kusungunuka mu DMSO
Phalala > Zaka ziwiri ngati zasungidwa bwino
Kupanga Mankhwala Mankhwalawa angapangidwe mu DMSO
Stock Solution yosungirako 0 - 4 C kwakanthawi kochepa (masiku mpaka masabata), kapena -20 C kwakanthawi (miyezi)

 


 

6. Ntchito Yachilengedwe - CAS: 959151-50-9aasraw

 

PF-750 ndiyodalirika, yodalira nthawi, yosasinthika FAAH inhibitor yokhala ndi ma IC50 0.6 ndi 0.016 μM mukamakonzedweratu ndi FAAH ya anthu yophatikizanso kwa mphindi 5 ndi 60, motsatana. Fatty acid amide hydrolase (FAAH) ndi ma enzyme omwe amachititsa hydrolysis ndikukhazikitsa mafuta amidi amidi kuphatikiza anandamide ndi oleamide. Zojambula pazochitika zosiyanasiyana zamatenda amtundu wa anthu ndi am'miyendo zidawulula kuti PF-750 imasankha kwambiri FAAH yokhudzana ndi ma serine hydrolases ena, osawonetsa zochitika zapadera mpaka 500 μM. PF-750 ikuwonetsa potency kabwinoko kuposa URB10 (Sigma # U597) pambuyo pa 4133 min preububation. PF-30 imasankha kwambiri FAAH. Ngakhale itafika 750 μM, idalibe kulumikizana ndi michere yambiri yoyesedwa, koma URB500 ndi ma inhibitors ena odziwika a FAAH sanachite bwino pakutsikira pang'ono (597 μM).

 

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

 


 

7. Kuwunikira kwa JZL-184aasraw

 

JZL-184 (1101854-58-3) ndi inhibitor yamphamvu komanso yosankha ya MAGL yokhala ndi IC50 ya 8 nM ndi 4 μM yoletsa MAGL ndi FAAH mu mbewa zamagulu a mbewa motsatana. Mtengo wa IC50: 8 nM Target: MAGL inhibitor mu vitro: JZL-184 imapangitsa DSE mu ma Purkinje neurons mu magawo a cerebellar ndi DSI mu CA1 pyramidal neurons m'magawo a hippocampal. JZL-184 ndiyamphamvu kwambiri poletsa mbewa MAGL kuposa makoswe MAGL. mu vivo: Mukaperekedwa kwa mbewa pa 16 mg / kg, intraperitoneally, JZL-184 imachepetsa magwiridwe antchito a MAGL ndi 85%, imakweza milingo yaubongo 2-AG ndi 8-fold, ndipo imapangitsa zochitika za analgesic m'mayeso osiyanasiyana opweteka omwe amatsanzira moyenera pakati cannabinoid (CB1) agonists. Kuwongolera koyipa kwa JZL-184 kwa FAAH (- / -) mbewa zidakulitsa kukula kwa gawo limodzi la mayankho a cannabimimetic, chithandizo chobwerezabwereza cha JZL-184 chidadzetsa kulolerana ndi zovuta zake, kulekerera kopitilira muyeso wazamankhwala wa cross-tetrahydrocannabinol, amachepetsa mu CB1 receptor agonist-yolimbikitsidwa guanosine 5'-O- (3 - [(35) S] thio) triphosphate kumanga, ndi kudalira monga zikuwonetsedwera ndi rimonabant-zomwe zimapangitsa kuti anthu azichotsa, mosasamala mtundu wawo.

 

JZL -184 NKHANI ZOPHUNZIRA
Dzina Lina JZL-184
chilinganizo chilinganizo
MW 520.5
gwero AASraw
CAS 1101854-58-3
Chiyeretso ≥98% (TLC)
Maonekedwe Chikasu cholimba
Kutupa Kusungunuka mu DMSO (10mg / ml)

 


 

8. Ntchito Yachilengedwe - CAS: 1101854-58-3aasraw

 

JZL-184 imaletsa MAGL, enzyme yomwe imayambitsa kutayika kwa endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide ndi 2-AG ndi endocannabinoids awiri amkati omwe amathandizira kulandira ma cannabinoid receptors CB1 ndi CB2. Anandamide imagwiritsidwa ntchito kwambiri ndi mafuta acid amide hydrolase (FAAH), pomwe monoacylglycerol lipase (MAGL) amaganiza kuti ndiye enzyme yomwe imayambitsa kuwonongeka kwa 2-AG. Ndizovuta kusiyanitsa zochita za awiriwa chifukwa ma inhibitors omwe amapezeka pano a MAGL sasankha, komanso amaletsa FAAH kapena ma enzyme ena. JZL-184 ndiye woyamba kusankha ma inhibitor a MAGL okhala ndi nanomolar portency komanso kupitilira 200 kusankha kwa MAGL vs FAAH. Mukapatsidwa mbewa, JZL-184 idakulitsa kuchuluka kwa 2-arachidonoylglycerol muubongo pafupifupi 8-fold, osakhudza magulu a anandamide.

 


 

9. Ma inhibitor osankha a monoacylglycerol lipase okhala ndi gulu lotakatakaaasraw

 

Matenda otchedwa 2-arachidonoyl glycerol (2-AG) ndi N-arachidonoyl ethanolamine (anandamide) amadetsedwa kwambiri ndi monoacylglycerol lipase (MAGL) ndi mafuta a acid amide hydrolase (FAAH). Kupezeka kwaposachedwa kwa O-aryl carbamates monga JZL-184 ngati MAGL inhibitors osankhidwa wathandiza kuti kufufuza ntchito za 2-AG ziwonetsedwe mu vivo. Komabe, JZL-184 ndi zina zotero za MAGL zowonongeka zikuwonetseratu zochitika zapamtunda za FAAH ndi zowona za carboxylesterases, zomwe zingasokoneze ntchito yawo mu maphunziro enaake. Pano, timalongosola gulu lapadera la carbamates la O-hexafluoroisopropyl (HFIP) lomwe limaletsa MAGL mu vitro ndi vivo ndi mphamvu yabwino komanso yosintha kwambiri, kuphatikizapo kusonyeza kuti palibe chochitika chokhalira ndi FAAH. Zofukufukuzi zimaphatikizapo ma carbamates a HFIP ngati mankhwala opangira mankhwala oletsera MAGL ndipo ayenera kulimbikitsa kufunafuna mavitamini ena omwe amachititsa kuti magulu otha kusokonezeka akufanana ndi magulu achilengedwe.

 


 

10. Kuwongolera pa buy JW-642 MAGL inhibitor sitepe ndi sitepeaasraw

 

• Google AASraw, lowani pa www.aasraw.com.
♦ Fufuzani JW-642 Powder (1416133-89-5) pa AASraw
• Pezani JW-642 Powder windows XP, ndi kulemba requirmnets anu.
♦ Timalandira imelo yanu ndikuyankhula zambiri.
 Tsimikizirani ndondomekoyi, ndipo malipiro athandizidwa ndipo tidzakonzekera katundu wobweretsera.

 


 

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