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MAGL inhibitor and FAAH Inhibitor : JW-642

& OL-135 & PF-750

MAGLinhibitorandFAAHInhibitor: JW-642&OL-135&PF-750............................................... 1
I.JW 642 basic Characters:.......................................................................................1
1. JW-642 Review.................................................................................................... 2
2. Biological Activity–CAS: 1416133-89-5............................................................... 3
3. OL-135 Review.....................................................................................................4
4. Biological Activity–CAS: 681135-77-3................................................................. 5
5. PF-750 Review..................................................................................................... 5
6. Biological Activity–CAS: 959151-50-9................................................................. 6
7. JZL-184 Review.................................................................................................... 7
8. Biological Activity–CAS: 1101854-58-3............................................................... 8
9. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group8
10. Guide on buy JW-642 MAGL inhibitor step by step.......................................... 9

I.JW 642 basic Characters:

Name: JW 642
CAS: 1416133-89-5
Molecular Formula: C21H20F6N2O3
Molecular Weight: 462.4
Melt Point:
Storage Temp: at -20°C 3 years Powder
Color: White solid

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1. JW-642 Review

JW-642 (1416133-89-5) is a potent, selective monoacylglycerol lipase (MAGL)

inhibitor with IC50 of 7.6, 14 and 3.7 nM for mouse, rat and human MAGL,
respectively. Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and
arachidonoyl ethanolamide are biologically active lipids that are involved in a
number of synaptic processes including activation of cannabinoid receptors.
Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis
of 2-AG to arachidonic acid and glycerol, thus terminating its biological function.
JW-642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50
values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain
membranes, respectively.1 JW-642 is selective for MAGL, requiring much higher
concentrations to effectively inhibit fatty acid amide hydrolase activity (IC50s = 31,
14, and 20.6 µM for mouse, rat, and human brain membranes, respectively).

JW-642 TECHNICAL DATA

Product name JW-642
CAS number 1416133-89-5
Formula C21H20F6N2O3
M.Wt 462.39
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical
A solution in methyl acetate
Appearance
Shipping Evaluation sample solution : ship with blue ice.All other available size: ship with RT ,
Condition or blue ice upon request
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the
General tips ultrasonic bath for a while.Stock solution can be stored below -20℃ for several
months.

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2. Biological Activity–CAS: 1416133-89-5

JW-642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50

values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain
membranes, respectively. IC50: 7.6/14/3.7 nM (mouse/rat/human MAGL)
Target: MAGL inhibitor JW-642 is selective for MAGL, requiring much higher
concentrations to effectively inhibit fatty acid amide hydrolase activity (IC50s = 31,
14, and 20.6 M for mouse, rat, and human brain membranes, respectively).

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3. OL-135 Review

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH.
OL-135 exhibits analgesic pharmacology in various animal models without the motor
impairment associated with direct CB1 agonism.FAAH Inhibitor OL-135 disrupts the
acquisition, but not consolidation, of contextual fear conditioning.Auditory fear
conditioning and shock reactivity remain unaffected.Together, these data suggest a
specific role for endocannabinoids in a subset of fear conditioning paradigms.

OL-135 TECHNICAL DATA

Product Name OL-135
CAS number 681135-77-3
Appearance Solid powder
Purity >98% (or refer to the Certificate of Analysis)
Shipped under ambient temperature as non-hazardous chemical. This product is
Shipping
stable enough for a few weeks during ordinary shipping and time spent in
Condition
Customs.
Storage Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term
Condition (months to years).
Solubility Soluble in DMSO, not in water
Shelf Life >2 years if stored properly
Drug
This drug may be formulated in DMSO
Formulation
Stock Solution
0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Storage

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4. Biological Activity–CAS: 681135-77-3

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH
devoid of CB1, CB2 and μ and δ opioid receptors activities that increases the
analgesic and hypothermic activity of anandamide

5. PF-750 Review
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and
inactivation of fatty acid amides including anandamide and oleamide. PF-750 is a
potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 and
0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes,
respectively.1 Activity-based profiling of various human and murine tissue proteome
samples revealed that PF-750 is highly selective for FAAH relative to other serine
hydrolases, showing no discernable off-site activity up to 500 µM.

PF-750 TECHNICAL DATA

Product name PF-750
CAS number 959151-50-9
Appearance Solid powder
Purity >98% (or refer to the Certificate of Analysis)
Shipped under ambient temperature as non-hazardous chemical. This product is
Shipping
stable enough for a few weeks during ordinary shipping and time spent in
Condition
Customs.
Storage Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term
Condition (months to years).
Solubility Soluble in DMSO
Shelf Life >2 years if stored properly
Drug
This drug may be formulated in DMSO
Formulation
Stock Solution
0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Storage

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6. Biological Activity–CAS: 959151-50-9

PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values 0.6
and 0.016 μM when preincubated with recombinant human FAAH for 5 and 60
minutes, respectively. Fatty acid amide hydrolase (FAAH) is the enzyme responsible
for hydrolysis and inactivation of fatty acid amides including anandamide and
oleamide. Activity-based profiling of various human and murine tissue proteome
samples revealed that PF-750 is highly selective for FAAH relative to other serine
hydrolases, showing no discernable off-site activity up to 500 μM. PF-750 shows
10-fold better potency than URB597 (Sigma# U4133) after 30 min preincubation.
PF-750 is highly selective on FAAH. Even at as high as 500 μM, it had no interactions
with many tested enzymes, but URB597 and other known FAAH inhibitors did not
perform well at low concentraction (100 μM).

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7. JZL-184 Review

JZL-184(1101854-58-3) is a potent and selective inhibitor of MAGL with IC50 of 8 nM

and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.
IC50 value: 8 nM Target: MAGL inhibitor in vitro: JZL-184 prolongs DSE in Purkinje
neurons in cerebellar slices and DSI in CA1 pyramidal neurons in hippocampal slices.
JZL-184 is more potent in inhibiting mouse MAGL than rat MAGL. in vivo: When
administered to mice at 16 mg/kg, intraperitoneally, JZL-184 reduces MAGL activity
by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety
of pain assays that qualitatively mimics direct central cannabinoid (CB1) agonists.
Acute administration of JZL-184 to FAAH(-/-) mice enhanced the magnitude of a
subset of cannabimimetic responses, repeated JZL-184 treatment led to tolerance to
its antinociceptive effects, cross-tolerance to the pharmacological effects of
Δ-tetrahydrocannabinol, decreases in CB1 receptor agonist-stimulated guanosine
5′-O-(3-[(35)S]thio)triphosphate binding, and dependence as indicated by
rimonabant-precipitated withdrawal behaviors, regardless of genotype.

JZL -184 TECHNICAL DATA

Alternative Name JZL-184
Formula Formula
MW 520.5
Source AASraw
CAS 1101854-58-3
Purity ≥98% (TLC)
Appearance Pale yellow solid
Solubility Soluble in DMSO (10mg/ml)

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8. Biological Activity–CAS: 1101854-58-3

JZL-184 selectively inhibits MAGL, the enzyme predominantly responsible for the
degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide
and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid
receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid
amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be
the enzyme primarily responsible for the degradation of 2-AG. It is difficult to
separate the activities of the two because most currently available inhibitors of
MAGL are not selective, and also inhibit FAAH or other enzymes. JZL-184 is the first
selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity
for MAGL vs FAAH. When administered to mice, JZL-184 increased levels of
2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of
anandamide.

9. Highly selective inhibitors of monoacylglycerol lipase

bearing a reactive group

The endocannabinoids 2-arachidonoyl glycerol (2-AG) and N-arachidonoyl

ethanolamine (anandamide) are principally degraded by monoacylglycerol lipase
(MAGL) and fatty acid amide hydrolase (FAAH), respectively. The recent discovery of
O-aryl carbamates such as JZL-184 as selective MAGL inhibitors has enabled
functional investigation of 2-AG signaling pathways in vivo. Nonetheless, JZL-184 and
other reported MAGL inhibitors still display low-level cross-reactivity with FAAH and
peripheral carboxylesterases, which can complicate their use in certain biological
studies. Here, we report a distinct class of O-hexafluoroisopropyl (HFIP) carbamates
that inhibits MAGL in vitro and in vivo with excellent potency and greatly improved
selectivity, including showing no detectable cross-reactivity with FAAH. These
findings designate HFIP carbamates as a versatile chemotype for inhibiting MAGL

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and should encourage the pursuit of other serine hydrolase inhibitors that bear
reactive groups resembling the structures of natural substrates.

10. Guide on buy JW-642 MAGL inhibitor step by step

♦ Google AASraw, enter into www.aasraw.com.

♦ Search JW-642 Powder(1416133-89-5) on AASraw
♦ Find out JW-642 Powder windows XP, and write down your requirmnets.
♦ We get your email and talk more details with you.
♦ Confirm the order, then payment done and we will arrange delivery goods for you
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