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Tlhahlobo ea 1.JW-642
Ketsahalo ea 2.Biological-CAS: 1416133-89-5
3.OL-135 Tlhahlobo
Ketsahalo ea 4.Biological-CAS: 681135-77-3
5. PF-750 Tlhahlobo
Ketsahalo ea 6.Biological-CAS: 959151-50-9
7. Tlhahlobo ea JZL-184
Ketsahalo ea 8.Biological-CAS: 1101854-58-3
9.Ha khethollang li-inhibitors tsa monoacylglycerol lipase tse nang le sehlopha se tsitsitseng
10.Guide ho reka JW-642 MAGL inhibitor mohato ka bohato


Video ea JW 642


I.JW 642 tsebo ea motheo:

Name: JW 642
CAS: 1416133-89-5
Molecular Formula: C21H20F6N2O3
Boima ba 'mele: 462.4
Melt Point:
Temp Temp Storage: ho -20 ° C lilemo tse 3 Powder
Color: Tšepe e tšoeu


1. Tlhahlobo ea JW-642aasraw

JW-642 (1416133-89-5) ke monoacylglycerol lipase e matla le e khethileng (MAGL) inhibitor e nang le IC50 ea 7.6, 14 le 3.7 nM bakeng sa mouse, rat le motho MAGL, ka ho latellana. Li-endocannabinoids tse kang 2-arachidonoyl glycerol (2-AG) le arachidonoyl ethanolamide li na le li-lipids tse sebetsang ka bongata tse kenyelletsang mekhoa e mengata ea synaptic e kenyeletsang ho amohela li-receptor tsa kankere. Monoacylglycerol lipase (MAGL) ke serine hydrolase e ikarabellang bakeng sa hydrolysis ea 2-AG ho arachidonic acid le glycerol, kahoo e felisa mosebetsi oa eona oa likokoana-hloko. JW-642 ke inhibitor e matla ea monoacylglycerol lipase (MAGL) e bontsang litsamaiso tsa IC50 tsa 7.6, 14, le 3.7 nM bakeng sa ho thibela MAGL ka mouse, rat, le lisele tsa motho tsa boko, ka ho latellana.1 JW-642 e khetha bakeng sa MAGL, e hlokang hore ho be le maemo a phahameng haholo ho thibela ka matla marotholi a mafura a amide hydrolase (IC50s = 31, 14, le XMUMX μM bakeng sa mouse, rat, le membrane ea boko ba motho, ka ho latellana).

JW-642 TLHALO TSA LINTHO TSE KOPITSOANG
lebitso Product JW-642
Nomoro ea CAS 1416133-89-5
riteloang C21H20F6N2O3
M.Wt 462.39
Solubility Ho qhibiliha ho DMSO> 10 mM Store Store -20 ° C
Ponahalo ea 'mele Tharollo ka methyl acetate
Ho romella boemo Hlahloba mohlala oa tharollo: sekepe se nang le leqhoa le leputsoa. ​​Boholo bo bong bo fumanehang: sekepe se nang le RT, kapa leqhoa le leputsoa ha le kōpa
Litlhahiso tse tloaelehileng Bakeng sa ho fumana metsi a mangata, ka kopo o futhumatsa tube ka 37 ℃ mme e sisinyehe ka ho sesa ka nako e telele. Solution ea motlakase e ka bolokoa ka tlase -20 ℃ ka likhoeli tse 'maloa.



Raw JW 642 phofo (1416133-89-5) hplc≥98% | Poda e ts'oanang


2. Mosebetsi oa Likokoana-CAS: 1416133-89-5aasraw

JW-642 ke inhibitor e matla ea monoacylglycerol lipase (MAGL) e bontsang litsamaiso tsa IC50 tsa 7.6, 14, le 3.7 nM bakeng sa ho thibela MAGL ka mouse, rat, le liphatsa tsa boko ba motho ka ho latellana. IC50: 7.6 / 14 / 3.7 nM (mouse / rat / motho MAGL)
Sepheo: MAGL inhibitor ea MAGL JW-642 e khetholla MAGL, e hlokang hore ho be le libaka tse phahameng haholo ho thibela mosebetsi o matla oa mafura a amide hydrolase (IC50s = 31, 14, le 20.6 M bakeng sa mouse, rat, le membrane ea boko ba motho ka ho latellana).


3. OL-135 Tlhahloboaasraw

OL-135 ke mokhatlo oa CNS, ea nang le matla a holimo le a khethiloeng ka mokhoa o tsitsitseng oa FAAH. OL-135 e bontša lipalo tsa liphoofolo tse fapaneng tsa liphoofolo tse sa tšoaneng tse nang le tšenyo ea motlakase e amanang le ho ikamahanya le bothata ba bothata bo botle ba AIDS.FAAH Inhibitor OL-1 e sitisa ho fumanoa, empa ha e kopane, ea boemo bo tšabehang ba boemo bo joalo.Hohloba ea ho tšaba le ho tsosoa ke ts'oaetso e ntse e sa amehe. data e fana ka maikutlo a karolo e khethehileng bakeng sa endocannabinoids ka karolo e itseng ea tšabo ea paradigms.

OL-135 TECHNICAL DATA
Name Product OL-135
Nomoro ea CAS 681135-77-3
Ponahalo Pfu e tiileng
Ho hloeka > 98% (kapa lebisa Certificate ea Tlhahlobo)
Ho romella boemo Li romelloa tlas'a mocheso o lekaneng e le lik'hemik'hale tse seng kotsi. Sehlahisoa sena se tsitsitse ka libeke tse 'maloa nakong ea thepa e tloaelehileng le nako e sebelisoang Mekhoeng.
Boemo Storage E omileng, e lefifi le ka 0 - 4 C ka nako e khutšoanyane (matsatsi ho isa ho libeke) kapa -20 C ka nako e telele (likhoeli ho isa ho lilemo).
Solubility Ho qhibiliha ka DMSO, eseng metsing
Shelf Life > Lilemo tse 2 haeba li bolokiloe hantle
Ho thehoa ha lithethefatsi Meriana ena e ka etsoa ka DMSO
Stock Tharollo Boloka 0 - 4 C ka nako e khutšoanyane (matsatsi ho isa ho libeke), kapa -20 C ka nako e telele (likhoeli)


4. Mosebetsi oa Likokoana-CAS: 681135-77-3aasraw

OL-135 ke motsoako oa CNS, ea nang le matla a maholo le a khethiloeng a amohelehang a FAAH ntle le CB1, CB2 le μ le δ opioid receptors mesebetsi e eketsang ts'ebetso ea analgesic le hypothermic ea anandamide.


5. PF-750 Tlhahloboaasraw

Fatty acid amide hydrolase (FAAH) ke enzyme e ikarabellang bakeng sa hydrolysis le ho hlahisa mafura a mafura a mafura a akarelletsang anandamide le oleamide. PF-750 ke ntho e matla, e itšetlehileng ka nako, e ke keng ea senngoa ka FAAH inhibitor e nang le litekanyetso tsa IC50 tsa 0.6 le 0.016 μM ha li etsoa ka pele ho FAAH ea batho bakeng sa 5 le 60 metsotso, ka ho latellana.1 Ts'ebetso e ts'oanang le ts'ebetso ea mefuta e fapa-fapaneng ea menyetla ea moriana ea motho le ea murine e senotsoe hore PF-750 e khetholla haholo FAAH ho tse ling tsa serine hydrolases, e bontšang ha ho na tšebetso e hlakileng ea ho etsa mosebetsi ho fihlela 500 μM.

PF-750 TLHALO TSA LINTHO TSE KOPITSOANG
lebitso Product PF-750
Nomoro ea CAS 959151-50-9
Ponahalo Pfu e tiileng
Ho hloeka > 98% (kapa lebisa Certificate ea Tlhahlobo)
Ho romella boemo Li romelloa tlas'a mocheso o lekaneng e le lik'hemik'hale tse seng kotsi. Sehlahisoa sena se tsitsitse ka libeke tse 'maloa nakong ea thepa e tloaelehileng le nako e sebelisoang Mekhoeng.
Boemo Storage E omileng, e lefifi le ka 0 - 4 C ka nako e khutšoanyane (matsatsi ho isa ho libeke) kapa -20 C ka nako e telele (likhoeli ho isa ho lilemo).
Solubility Ho qhibiliha ho DMSO
Shelf Life > Lilemo tse 2 haeba li bolokiloe hantle
Ho thehoa ha lithethefatsi Meriana ena e ka etsoa ka DMSO
Stock Tharollo Boloka 0 - 4 C ka nako e khutšoanyane (matsatsi ho isa ho libeke), kapa -20 C ka nako e telele (likhoeli)


6. Mosebetsi oa Likokoana-CAS: 959151-50-9aasraw

PF-750 ke ntho e matla, e itšetlehileng ka nako, e sa tsitseng FAAH inhibitor e nang le litekanyetso tsa IC50 0.6 le 0.016 μM ha li etsoa ka pele ho FAAH ea batho bakeng sa 5 le 60 metsotso ka ho latellana. Fatty acid amide hydrolase (FAAH) ke enzyme e ikarabellang bakeng sa hydrolysis le ho hlahisa mafura a mafura a mafura a akarelletsang anandamide le oleamide. Tlaleho e thehiloeng mesebetsing ea mefuta e sa tšoaneng ea lisele tsa proteome ea batho le ea moriana e senola hore PF-750 e khetholla haholo ho FAAH ho feta serine hydrolases, e bonts'ang tšebetso e sa hlokomelehang ea mobu ho fihlela 500 μM. PF-750 e bontsa potenteng ea 10 hamolemo ho feta URB597 (Sigma # U4133) kamora 30 min pele ho lihlopha. PF-750 e khetholla haholo ho FAAH. Esita le ka holimo ho 500 μM, e ne e sa sebelisane le li-enzyme tse ngata tse lekiloeng, empa URB597 le tse ling tse tsebahalang tsa FAAH inhibitors ha lia ka tsa sebetsa hantle ka li-concentrating (100 μM).

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


7. Tlhahlobo ea JZL-184aasraw

JZL-184 (1101854-58-3) ke inhibitor e matla le e khethileng ea MAGL le IC50 ea 8 nM le 4 μM bakeng sa ho thibela MAGL le FAAH ka liphatsa tsa moriana tsa boko. C50 bohlokoa: 8 NM Target: MAGL inhibitor in vitro: JZL-184 nako e telele DSE ka Purkinje neurons ka cerebellar dilae le DSI ka CA1 pyramidal neurons li-hippocampal lilae. JZL-184 e matla haholo ho thibela mouse MAGL ho feta rat MAGL. ka vivo: Ha o fuoa litoeba tsa 16 mg / kg, ka nako e sa lekanyetsoang, JZL-184 e fokotsa mosebetsi oa MAGL ka 85%, e phahamisa maemo a bokooa a 2-AG ka 8, mme e etsa mosebetsi oa analgesic ka litlhahlobo tse sa tšoaneng tse nang le litsela tse sa tšoaneng Central Cannabinoid (CB1) li-agonists. Ho tsamaisoa ha JZL-184 hantle ho FAAH (- / -) litoeba li ntlafalitse boholo ba likarabo tsa cannabimimetic, phetoho e phetoang ea JZL-184 e lebisitseng ho mamellana le liphello tsa eona, ho mamellana ha sepakapaka le liphello tsa pharmacological tsa D-tetrahydrocannabinol, ho fokotseha ho CB1 receptor agonist-e tsositse guanosine 5'-O- (3 - [(35) S] thio) e tlamang triphosphate, le ho itšetleha joalokaha ho bontšoa ke boitšoaro bo hlephileng ba ho tlohela, ho sa tsotellehe li-genotype.

JZL -184 LITABA TSE LING
Lebitso le leng JZL-184
riteloang riteloang
MW 520.5
mohloli o moholo AASraw
CAS 1101854-58-3
Ho hloeka ≥98% (TLC)
Ponahalo Pale e mongobo e thata
Solubility Ho qhibiliha ka DMSO (10mg / ml)


8. Mosebetsi oa Likokoana-CAS: 1101854-58-3aasraw

JZL-184 e khetha ho thibela MAGL, e leng mohloli o moholo oa lik'hemik'hale tse nang le boikarabelo haholo bakeng sa ho silafala ha 2-arachidonoylglycerol (2-AG). Anandamide le 2-AG ke li-endocannabinoid tse peli tse mamellang li-receptors tsa kannete CB1 le CB2. Anandamide e na le metsoli e nang le mafura a mafura a amide hydrolase (FAAH), athe monoacylglycerol lipase (MAGL) ho nahanoa hore ke enzyme e ikarabellang ka ho senyeha ha 2-AG. Ho thata ho arola mesebetsi ea bobeli hobane hangata li-inhibitors tsa MAGL ha li khetholle, hape li thibela FAAH kapa li-enzyme tse ling. JZL-184 ke khetho ea pele ea inhibitor ea MAGL e nang le boikutlo ba nanomolar le ho feta 200-selectivity bakeng sa MAGL vs FAAH. Ha ho sebelisoa litoeba, JZL-184 e eketsehile maemong a 2-Arachidonoylglycerol bokoeng ka hoo e ka bang 8, e se nang phello maemong a anandamide.


9. Li-inhibitor tse phahameng tsa monoacylglycerol lipase tse nang le sehlopha se tsitsitsengaasraw



Li-endocannabinoids 2-arachidonoyl glycerol (2-AG) le N-arachidonoyl ethanolamine (anandamide) li hlile li silafatsoa ke monoacylglycerol lipase (MAGL) le mafura a acid amide hydrolase (FAAH). Ho sibolloa ha morao-rao ha li-aryl carbamates tse kang JZL-184 e le MAGL inhibitors e khethileng e entse hore lipatlisiso tsa mesebetsi ea 2-AG li be teng ka har'a lipapatso. Leha ho le joalo, JZL-184 le tse ling tse tlalehiloeng tsa MAGL inhibitors li ntse li bontša mekhoa e tlaase ea ho feto-fetoha le FAAH le methapo ea carboxylesterase, e leng e ka kenyelletsang tšebeliso ea tsona liphuputsong tse itseng tsa likokoana-hloko. Mona, re tlaleha sehlopha se ikhethang sa li-carbamate tsa O-hexafluoroisopropyl (HFIP) tse thibelang MAGL in vitro le vivo ka mokhoa o babatsehang oa potency le ho ntlafatsa haholo selectivity, ho kenyeletsa ho bontša hore ha ho bonahale eka ho na le cross-reactivity le FAAH. Liphuputso tsena li hlalosa lik'hemik'hale tsa HFIP e le lik'hemik'hale tse nang le mekhoa e metle bakeng sa ho thibela MAGL 'me li lokela ho khothaletsa ho phehella li-serine hydrolase tse ling tse nang le likokoana-hloko tse nang le lihlopha tse sebetsang hantle tse tšoanang le mehaho ea limela tsa tlhaho.


10. Tataiso ea ho reka JW-642 MAGL inhibitor mohato ka mohatoaasraw

♦ Google AASraw, kena ho www.aasraw.com.
♦ Batla Powder ea JW-642 (1416133-89-5) ho AASraw
♦ Fumana Powder ea JW-642 lifensetere tsa XP, ebe o ngola requirmnets tsa hau.
♦ Re fumana imeile ea rona mme re bua lintlha tse ling le uena.
♦ Tiisa taelo eo, joale tefo e etsoa mme re tla hlophisa thepa ea thepa bakeng sa hau hamorao.


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