MAGL taofiofia ma FAAH Inhibitor: JW-642 & OL-135 & PF-750 丨 AASraw
AASraw gaosia Cannabidiol (CBD) paʻu ma Hemp Taua Suauʻu tele!

 

Mea uma e uiga i le Mibolerone (Siaki lau)

 

  1.JW-642 Toe Iloiloga
  2.Giological Action – CAS: 1416133-89-5
  3.OL-135 Toe Iloiloga
  4.Giological Action – CAS: 681135-77-3
  5. PF-750 Iloiloga
  6.Giological Action – CAS: 959151-50-9
  7. JZL-184 Iloiloga
  8.Giological Action – CAS: 1101854-58-3
  9.O le mea e sili atu i le initaneti filifilia o le monoacylglycerol lipase o loʻo tauaveina ai se kulupu faʻamalosi
  10.Guide ile faʻatau ole JW-642 MAGL taofi laʻasaga ile laʻasaga

 


 

JW 642 video

 

 


 

I.JW 642 Uiga masani:

 

igoa: JW 642
CAS: 1416133-89-5
Fua Faatatau Molecular: C21H20F6N2O3
Pauna Molecular: 462.4
Melt Point:
Teu o le Teuina: i -20 ° C 3 tausaga Malosiaga
Valivali: Paʻepaʻe papaʻe

 


 

1. JW-642 Toe Iloilogaaasraw

 

JW-642 (1416133-89-5) o se malosi, filifilia monoacylglycerol lipase (MAGL) mea faʻatamaina ma IC50 o 7.6, 14 ma 3.7 nM mo isumu, isumu ma tagata MAGL, faʻatulagaina. Endocannabinoids pei o le 2-arachidonoyl glycerol (2-AG) ma le arachidonoyl ethanolamide o ni meaola o loʻo galue i lipine o loʻo aʻafia i le tele o synaptic gaioiga e aofia ai le faʻagaina o le cannabinoid. Monoacylglycerol lipase (MAGL) o se serine hydrolase e nafa ma le faʻamamaina o le 2-AG i le arachidonic acid ma le glycerol, ma faʻamutaina ai lona faʻagaioiga o meaola. O le JW-642 o se malosi e taofiofi ai le monoacylglycerol lipase (MAGL) o loʻo faʻaalia ai le taua o le IC50 o le 7.6, 14, ma le 3.7 nM mo le taofiofia o le MAGL i isumu, isumu ma le faiʻai o le tagata, e tusa ai ma lea ituaiga. O le JW-1 e filifilia mo le MAGL. manaʻomia tele maualuga faʻasologa e lelei taofiofia gaʻo acid amide hydrolase gaioiga (IC642s = 50, 31, ma le 14 µM mo isumu, isumu, ma tagata faiʻai membrane, faasologa).

 

JW-642 TECHNICAL DATA
igoa oloa JW-642
Numera CAS 1416133-89-5
fomula C21H20F6N2O3
M.Wt 462.39
Solubility Soluble i le DMSO> 10 mM Teuina Faleoloa i -20 ° C
Vaaiga Faaletino O se vaifofo i le methyl acetate
Vaa Iloiloga faʻataʻitaʻiga: folau faʻatasi ma le aisa lanu moana. Isi lava avanoa: uta faʻatasi ma le RT, poʻo le aisa lanumoana i luga o se talosaga
Fautuaga lautele Mo le mauaina o se maualuga maualuga, faamolemole faamanafana le paipa i le 37 ℃ ma lulu i le ultrasonic bath mo sina taimi. E mafai ona teuina i lalo -20 ℃ mo ni nai masina.

 

Laoa JW 642 (1416133-89-5) hplc≥98% | Laʻau o le AASraw

 


 

2. Gaioiga Faʻafaʻanatura – CAS: 1416133-89-5aasraw

 

O le JW-642 ose malosiʻaga taofiofi o le monoacylglycerol lipase (MAGL) e faʻaalia ai le taua o le IC50 o le 7.6, 14, ma le 3.7 nM mo le taofiofia o le MAGL i isumu, isumu ma le faiʻai o le tagata. IC50: 7.6 / 14 / 3.7 nM (isumu / isumu / tagata MAGL)
Manulauti: O le MAWL inhibitor JW-642 ua filifilia mo le MAGL, e manaʻomia ai le maualuga o faʻasalalauga e faʻamalosi ai le gaosiga o le fatty acid amide hydrolase activity (IC50s = 31, 14, ma le 20.6 M mo le kiore, leki, ma le faiʻai o le faiʻai o tagata.).

 


 

3. OL-135 Toe Iloilogaaasraw

 

Ole OL-135 o le CNS penetrant, sili ona malosi ma filifilia le inhibitor faʻafouina o FAAH. OL-135 o loʻo faʻaalia togafitiga faʻapitoa i vailaʻau o manu eseese e aunoa ma le afaina o le moto e fesootai ma CB1 agonism.FAAH Inhibitor OL-135 faʻalavelaveina le mauaina, ae le o le faʻamalosia, o le fefefe i le tulaga. faʻamatalaga e taʻu mai ai se matafaioi faapitoa mo le endocannabinoids i se vaega o le fefefe e faʻatulagaina mea faʻapitoa.

 

OL-135 TECHNICAL DATA
Igoa oloa OL-135
Numera CAS 681135-77-3
Faʻaaliga Paʻu paʻu
Mama Atoatoa i Tulaga > 98% (pe faʻasino i le Tusi Faʻamaonia o Suʻesuʻega)
Vaa Sueina i lalo o le vevela mafanafana o vailaau e leai se lamatiaga. O lenei oloa e lava ma totoe mo ni nai vaiaso aʻo faʻaaogaina masani ma taimi faʻaalu i le Ofisa o Tiute.
teuina o Meaai a Tuutuuga Faʻamago, pogisa ma i le 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso) poʻo le -20 C mo se taimi umi (masina i tausaga).
Solubility Soluble i le DMSO, ae le o le vai
Shelf Life > 2 tausaga pe a fai e teu lelei
Faiga o vailaʻau O lenei vailaau faasaina e mafai ona fausia i le DMSO
Faʻamaumauga Faʻatau Mea 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso), poʻo le -20 C mo se taimi umi (masina)

 

 


 

4. Gaioiga Faʻafaʻanatura – CAS: 681135-77-3aasraw

 

OL-135 o le CNS penetrant, sili ona malosi ma le filifili filifilia o le FAAH e aunoa ma gaoioiga a CB1, CB2 ma μ ma δ opioid ia e faʻapupulaina ai le faʻamaʻi ma le isi mea o le gasegase.

 


 

5. PF-750 Iloilogaaasraw

 

Fatty acids amide hydrolase (FAAH) o le enzyme e nafa ma le gataifale ma le faʻaaogaina o amides amy acid e aofia ai le faʻasalaga ma le faʻatau. O le PF-750 o se tagata malosi, faʻalagolago i le taimi, faʻafitia le FAAH i le IC50 o 0.6 ma 0.016 μM pe a faʻapipiʻiina FAAH mo le 5 ma le 60 minute, i le faasologa .1 Faʻavasegaina o galuega eseese o tagata puipui ma tagata puipui o le PF-750 e sili ona filifilia mo le FAAH e fesoʻotaʻi ma isi serine hydrolases, e le faʻaalia ai se gaoioiga e le mafai ona faʻasalalau ile 500 μM.

 

PF-750 TECHNICAL DATA
igoa oloa PF-750
Numera CAS 959151-50-9
Faʻaaliga Paʻu paʻu
Mama Atoatoa i Tulaga > 98% (pe faʻasino i le Tusi Faʻamaonia o Suʻesuʻega)
Vaa Sueina i lalo o le vevela mafanafana o vailaau e leai se lamatiaga. O lenei oloa e lava ma totoe mo ni nai vaiaso aʻo faʻaaogaina masani ma taimi faʻaalu i le Ofisa o Tiute.
teuina o Meaai a Tuutuuga Faʻamago, pogisa ma i le 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso) poʻo le -20 C mo se taimi umi (masina i tausaga).
Solubility Soluble i le DMSO
Shelf Life > 2 tausaga pe a fai e teu lelei
Faiga o vailaʻau O lenei vailaau faasaina e mafai ona fausia i le DMSO
Faʻamaumauga Faʻatau Mea 0 - 4 C mo se taimi puʻupuʻu (aso i vaiaso), poʻo le -20 C mo se taimi umi (masina)

 


 

6. Gaioiga Faʻafaʻanatura – CAS: 959151-50-9aasraw

 

PF-750 o se malosi, faʻalagolago i le taimi, le mafai ona toe faʻaleleia FAAH ma IC50 taua 0.6 ma 0.016 μM pe a preincubated ma recombinant tagata FAAH mo 5 ma 60 minute, faʻatulagaina. Fatty acid amide hydrolase (FAAH) o le enzyme nafa ma hydrolysis ma le toaga o fatty acid amides e aofia ai le anandamide ma le oleamide. Gaioiga-faʻavae faʻamaumauga o le tele o tagata ma murine pepa solo proteome faʻataʻitaʻiga faʻaalia ai o le PF-750 e sili ona filifilia mo le FAAH e faʻatatau i isi serine hydrolases, e le faʻaaliaina se gaioiga i fafo atu o le gaioiga oʻo atu i le 500 μM. PF-750 faʻaalia le 10-gaugau sili atu le malosi nai lo URB597 (Sigma # U4133) i le maeʻa ai o le 30 min preincubation. PF-750 e sili ona filifilia ile FAAH. E oʻo lava i le maualuga e pei o le 500 μM, e leai ni fesoʻotaʻiga ma le tele o suʻesuʻeina o enzyme, ae o le URB597 ma isi lauiloa FAAH na taofia na le faʻamalieina lelei i le maualalo o le faʻasologa (100 μM).

 

MAGL taofiofia ma FAAH Inhibitor JW-642 & OL-135 & PF-750

 


 

7. JZL-184 Iloilogaaasraw

 

O le JZL-184 (1101854-58-3) ose tagata malosi na te taofiofi le MAGL ma le IC50 o le 8 nM ma le 4 μM mo le taofiofia o le MAGL ma le FAAH i totoga o le faiai o le faiʻai. Taua IC50: 8 nM Taunuʻuga: MAGL mea taofiofia i vitro: JZL-184 faʻaumiumi DSE i Purkinje neo i cerebellar fasi ma DSI i CA1 pyramidal neuron i hippocampal fasi. JZL-184 e sili atu le malosi i le taofiofia o le isumu MAGL nai lo rat MAGL. in vivo: A faʻatautaia i isumu i le 16 mg / kg, faʻasolosolo, JZL-184 faʻaititia MAGL gaioiga e 85%, siitia faiaʻoga 2-AG tulaga e 8-lafu, ma elicits analgesic gaioiga i le tele o tiga tofotofoga e faʻataʻitaʻi faʻataʻitaʻi faʻataʻitaʻi ogatotonu cannabinoid (CB1) agonists. Ogaoga pulega o JZL-184 ia FAAH (- / -) isumu faʻateleina le tele o se vaega o tali cannabimimetic, faifai pea JZL-184 togafitiga taʻitaʻia le faapalepale i ona antinociceptive aafiaga, koluse-faʻapalepale i le vailaʻau aafiaga o le Δ-tetrahydrocannabinol, faaitiitia i le CB1 receptor agonist-stimulated guanosine 5'-O- (3 - [(35) S] thio) triphosphate fusifusia, ma le faʻalagolago e pei ona faʻailoa mai e rimonabant-faʻatapulaʻaina le faʻateʻaina o amioga, tusa lava pe o le a le genotype.

 

JZL -184 FUAFUAGA FAʻAVAE
Isi Igoa JZL-184
fomula fomula
MW 520.5
puna AASraw
CAS 1101854-58-3
Mama Atoatoa i Tulaga ≥98% (TLC)
Faʻaaliga Paʻe samasama maʻa
Solubility Soluble i le DMSO (10mg / ml)

 


 

8. Gaioiga Faʻafaʻanatura – CAS: 1101854-58-3aasraw

 

O le JZL-184 e filifili faʻasolitulafono le MAGL, o le enzyme e tele nafa ma le faʻaleagaina o le endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide ma le 2-AG o i latou ia endogenous endocannabinoids e faʻagaoioia le mauaina cannabinoid CB1 ma CB2. O le Anandamide e tele na gaosia e le fatty acid amide hydrolase (FAAH), ae o le monoacylglycerol lipase (MAGL) e manatu o le enzyme e mafua ai le faʻaleagaina o le 2-AG. E faigata ona tuʻu eseʻese gaioiga a mea ia e lua ona o le tele o taimi nei o loʻo avanoa nei mea e taofia ai le MAGL e le filifilia, ma e faʻatamaia ai foi le FAAH poʻo isi fualaʻau. JZL-184 o le muamua filifilia filifilia o le MAGL ma nanomolar portency ma sili atu i le 200-fold selectivity mo MAGL vs FAAH. A faʻatonuina i isumu, JZL-184 faʻateleina tulaga o le 2-arachidonoylglycerol i le faiʻai e tusa o le 8-lafu, ma leai se aʻafiaga i tulaga o le anandamide.

 


 

9. O tagata e taofiofi filifilia o le monoacylglycerol lipase e maua mai ai le kulupu e toe faʻaola maiaasraw

 

O le endocannabinoids 2-arachidonoyl glycerol (2-AG) ma le N-arachidonoyl ethanolamine (anandamide) e matua faaleagaina e le monoacylglycerol lipase (MAGL) ma le fatty acid amide hydrolase (FAAH), i le faasologa. O le mauaina talu ai nei o le O-aryl carbamates e pei o le JZL-184 o ni tagata inhibitors MAGL filifilia ua mafai ai le suʻesuʻeina o galuega a 2-AG ala i signo. Ae ui i lea, o le JZL-184 ma isi inhibitors MAGL ua lipotia mai o loʻo faʻaalia pea le faʻafetauia o le cross-reactivity ma le FAAH ma le lautele o carboxylesterases, lea e mafai ona faʻaaogaina ai lo latou faʻaaogaina i nisi suʻesuʻega faʻaletagata. I lenei, tatou te lipotia se vasega manino o le O-hexafluoroisopropyl (HFIP) carbamates e inhibits MAGL in vitro ma ola ai i se tulaga sili ona lelei ma faaleleia ai le filifilia, e aofia ai le leai o se gasegase e mafai ona iloagofie ma le FAAH. O nei suʻesuʻega ua taʻua ai le HFIP carbamates e avea o se faʻataʻitaʻiga faʻapitoa mo le faʻasaina o le MAGL ma e tatau ona faʻamalosia le tulituliloaina o isi inhibitors serine hydrolase o loʻo i ai ni vaega faʻamautu e foliga tutusa ma le fausaga o mea faʻapitoa.

 


 

10. Taʻiala ile faʻatau ole JW-642 MAGL taofi laasaga i lea laasagaaasraw

 

♦ Google AASraw, ulufale i le www.aasraw.com.
♦ Suʻe le JW-642 Powder (1416133-89-5) i le AASraw
♦ Saili JW-642 efuefu faamalama XP, ma tusi i lalo au tusi talosaga.
♦ Matou te mauaina lau imeli ma talanoa faʻamatalaga faʻatasi ma oe.
♦ Faamaonia le poloaiga, ona totogi lea ma o le a matou faʻapipiʻiina faʻapipiʻi oloa mo oe mulimuli ane.

 


 

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