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Zotsatira za 1.JW-642
Ntchito ya 2.Biological-CAS: 1416133-89-5
Zotsatira za 3.OL-135
Ntchito ya 4.Biological-CAS: 681135-77-3
5. PF-750 Review
Ntchito ya 6.Biological-CAS: 959151-50-9
7. JZL-184 Review
Ntchito ya 8.Biological-CAS: 1101854-58-3
9.Masewera osankhidwa a monoacylglycerol lipase omwe amachititsa gulu lokhazikika
10.Guide kugula JW-642 MAGL inhibitor pang'onopang'ono


JW 642 kanema


I.JW 642 Anthu oyambirira:

Name: JW 642
CAS: 1416133-89-5
Makhalidwe a Maselo: 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 monoacylglycerol lipase (MAGL) inhibitor yamphamvu kwambiri, yomwe imakhala ndi IC50 ya 7.6, 14 ndi 3.7 nM ya mbewa, makoswe komanso MAGL anthu. Matenda otchedwa epocannabinoids monga 2-arachidonoyl glycerol (2-AG) ndi arachidonoyl ethanolamide ndi zamoyo zamagetsi zomwe zimaphatikizapo njira zosiyanasiyana monga kuphatikizidwa kwa mapuloteni. Monoacylglycerol lipase (MAGL) ndi serine hydrolase yomwe imayambitsa hydrolysis ya 2-AG kwa arachidonic asidi ndi glycerol, motero zimathetsa mphamvu zake. JW-642 ndizowononga kwambiri monoacylglycerol lipase (MAGL) yomwe imasonyeza machitidwe a IC50 a 7.6, 14, ndi 3.7 nM chifukwa choletsa MAGL mu mbewa, makoswe, ndi ubongo waumunthu .1 JW-642 imasankha MAGL, kufunika kwambiri kuti zikhale zotetezeka kwambiri kuti ziletsa mafuta a asidi amadzi hydrolase ntchito (IC50s = 31, 14, ndi 20.6 μM chifukwa cha mbewa, makoswe, ndi ubongo waumunthu).

JW-642 ZOKHUDZA ZOTHANDIZA
dzina mankhwala JW-642
Nambala ya CAS 1416133-89-5
chilinganizo C21H20F6N2O3
M.Wt 462.39
Kutupa Kusungunuka mu DMSO> 10 mM Kusungirako Kusungirako ku -XUMUM ° 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 njira yowonongeka ya monoacylglycerol lipase (MAGL) yomwe imasonyeza machitidwe a IC50 a 7.6, 14, ndi 3.7 nM chifukwa choletsa MAGL mu mbewa, makoswe, ndi ubongo waumunthu. IC50: 7.6 / 14 / 3.7 nM (mbewa / makoswe / anthu MAGL)
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 kutanthauza Certificate of Analysis)
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 Dry, mdima ndi 0 - 4 C kwa nthawi yochepa (masiku mpaka masabata) kapena -20 C kwa nthawi yaitali (miyezi mpaka zaka).
Kutupa Kusungunuka mu DMSO, osati m'madzi
Phalala > Zaka 2 ngati zasungidwa bwino
Kupanga Mankhwala Mankhwalawa angapangidwe mu DMSO
Stock Solution yosungirako 0 - 4 C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 C kwa nthawi yaitali (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. PF-750 Reviewaasraw

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 kutanthauza Certificate of Analysis)
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 Dry, mdima ndi 0 - 4 C kwa nthawi yochepa (masiku mpaka masabata) kapena -20 C kwa nthawi yaitali (miyezi mpaka zaka).
Kutupa Kusungunuka mu DMSO
Phalala > Zaka 2 ngati zasungidwa bwino
Kupanga Mankhwala Mankhwalawa angapangidwe mu DMSO
Stock Solution yosungirako 0 - 4 C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 C kwa nthawi yaitali (miyezi)


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

PF-750 ndi yodalirika, yodalira nthawi, yosasinthika FAAH inhibitor yokhala ndi IC50 miyezo 0.6 ndi 0.016 μM pamene imayambitsidwa ndi FAAH yowonjezera kwa 5 ndi 60 maminiti. Fatty acid amide hydrolase (FAAH) ndiyo nyamayi yomwe imayambitsa hydrolysis ndi kusokoneza mafuta amchere amide kuphatikizapo anandamide ndi oleamide. Zotsatira zochitidwa ndi ntchito za mitundu yosiyanasiyana ya anthu ndi minofu za proteome zatsimikizira kuti PF-750 imasankha kwambiri FAAH ndi zina zotchedwa serine hydrolases, zosonyeza kuti palibe ntchito yodalirika yomwe ikuchitika mpaka 500 μM. PF-750 ikuwonetsa 10 mphindi yabwino kuposa URB597 (Sigma # U4133) pambuyo pa 30 min. PF-750 imasankha kwambiri pa FAAH. Ngakhale ngakhale ngati 500 μM, sizinayanjane ndi michere yambiri yoyesedwa, koma URB597 ndi zina zotchedwa FAAH inhibitors sizinachite bwino pamtunda wochepa (100 μM).

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


7. JZL-184 Reviewaasraw

JZL-184 (1101854-58-3) ndi njira yowonongeka ya MAGL ndi IC50 ya 8 nM ndi 4 μM chifukwa choletsa MAGL ndi FAAH mu makoswe a ubongo. Mtengo wa IC50: 8 NM Target: MAGL inhibitor mu vitro: JZL-184 yaitali DSE mu Purkinje ndiurons mu cerebellar magawo ndi DSI mu CA1 pyramidal neurons mu hippocampal magawo. JZL-184 ndizowonjezereka kwambiri poletsa HIV MAGL kuposa makoswe MAGL. mu vivo: Pogwiritsidwa ntchito kwa mbewa pa 16 mg / kg, intraperitoneally, JZL-184 imachepetsa ntchito ya MAGL ndi 85%, imakweza maonekedwe a ubongo 2-AG ndi 8, ndipo imapanga ntchito ya analgesic m'mayesero osiyanasiyana opweteka omwe amatsanzira molondola midzi yamagetsi (CB1) agonists. Kuwongolera bwino kwa JZL-184 kwa FAAH (- / -) mbewa zinapangitsa kukula kwa gawo la maynabimimetic mayankho, katchulidwe ka JZL-184 kawiri kawiri kamene kanapangitsa kuti asamalimbikitsane ndi zotsatira zake, kulekerera pamtundu wa mankhwala a Δ-tetrahydrocannabinol, kuchepa mu CB1 receptor agonist-analimbikitsa guanosine 5'-O- (3 - [(35) S] thio) triphosphate kumangirira, ndi kudalira monga momwe ziwonetsedwera ndi khalidwe lochotsa khalidwe lopanda mphamvu, mosasamala kanthu za mtundu wa majeremusi.

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 imalepheretsa MAGL, yomwe imayambitsa matendawa makamaka chifukwa cha kuwonongeka kwa matenda a 2-arachidonoylglycerol (2-AG). Anandamide ndi 2-AG ndiwo awiri omwe amachititsa kuti mapuloteni a CB1 ndi CB2 asamalire. Anandamide amadziwika kwambiri ndi mafuta a asidi amadzi hydrolase (FAAH), pamene monoacylglycerol lipase (MAGL) amaganiza kuti ndi enzyme makamaka yomwe imayambitsa kuwonongeka kwa 2-AG. N'zovuta kupatukana ntchito ziwirizi chifukwa zamakono zomwe zimapezeka mu MAGL sizisankha, komanso zimalepheretsa FAAH kapena mavitamini ena. JZL-184 ndiyo yoyamba inhibitor ya MAGL ndi chidziwitso cha nanomolar komanso pa 200-selectivity kwa MAGL vs FAAH. Pogwiritsidwa ntchito kwa mbewa, JZL-184 inakula kuchuluka kwa 2-arachidonoylglycerol mu ubongo pafupi ndi 8 pokha, popanda zotsatira pamagulu a anandamide.


9. Makina otetezera kwambiri a monoacylglycerol lipase akukhala ndi gulu lokhazikikaaasraw



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. Zotsatira pa kugula JW-642 MAGL inhibitor sitepe ndi sitepeaasraw

• Google AASraw, lowani pa www.aasraw.com.
Fufuzani Powder JW-642 (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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