Ugrás a tartalomra
Merck

SML2732

Sigma-Aldrich

DO34

≥98% (HPLC)

Szinonimák:

(2-Benzyl-4-{[(2-methyl-2-propanyl)oxy]carbonyl}piperazinyl){4-[(4-trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl}methanone, 3-(Phenylmethyl)-4-[[4-[4-(trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl]carbonyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez


About This Item

Tapasztalati képlet (Hill-képlet):
C26H28F3N5O4
CAS-szám:
Molekulatömeg:
531.53
MDL-szám:
UNSPSC kód:
12352200
NACRES:
NA.77

Minőségi szint

Teszt

≥98% (HPLC)

form

powder

szín

white to beige

oldhatóság

DMSO: 2 mg/mL, clear

tárolási hőmérséklet

−20°C

SMILES string

O=C(N1CCN(CC1CC2=CC=CC=C2)C(OC(C)(C)C)=O)N3N=NC(C4=CC=C(C=C4)OC(F)(F)F)=C3

Biokémiai/fiziológiai hatások

DO34 is a brain-penetrant, selective and highly potent diacylglycerol lipase inhibitor (recom human DAGLα/β pIC50 = 8.2/8.1 by SAG hydrolysis; mouse brain DAGLα/β pIC50 = 9.1-9.3/8.6 by ABPP ReDiMe) with detectable off-target activity toward only ABHD6 & PLA2G7 among all mouse brain serine hydrolases and little affinity toward cannabinoid receptors CB1/2. DO34 blocks depolarization-induced suppression of excitation (DSE IC50 = 0.18 μM) and inhibition (100% DSI blockage at 1 μM) in mouse cerebellar and hippocampal slices ex vivo, and attenuate LPS-induced neuroinflammatory responses by lowering brain 2-AG & PGE2 level in mice in vivo (50 mg/kg, i.p).

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable


Analitikai tanúsítványok (COA)

Analitikai tanúsítványok (COA) keresése a termék sarzs-/tételszámának megadásával. A sarzs- és tételszámok a termék címkéjén találhatók, a „Lot” vagy „Batch” szavak után.

Már rendelkezik ezzel a termékkel?

Az Ön által nemrégiben megvásárolt termékekre vonatkozó dokumentumokat a Dokumentumtárban találja.

Dokumentumtár megtekintése

Xiaojie Liu et al.
Scientific reports, 6, 35829-35829 (2016-10-25)
The endocannabinoid 2-arachidonoylglycerol (2-AG) mediates retrograde synaptic depression including depolarization-induced suppression of excitation (DSE) and inhibition (DSI). 2-AG is degraded primarily by monoacylglycerol lipase (MAGL), which is expressed in neurons and astrocytes. Using knockout mice in which MAGL is deleted
Hui Deng et al.
Journal of medicinal chemistry, 60(1), 428-440 (2016-12-20)
Triazole ureas constitute a versatile class of irreversible inhibitors that target serine hydrolases in both cells and animal models. We have previously reported that triazole ureas can act as selective and CNS-active inhibitors for diacylglycerol lipases (DAGLs), enzymes responsible for
Jayme R McReynolds et al.
Biological psychiatry, 84(2), 85-94 (2017-11-05)
Clinical reports suggest that rather than directly driving cocaine use, stress may create a biological context within which other triggers for drug use become more potent. We hypothesize that stress-induced increases in corticosterone "set the stage" for relapse by promoting
Carol A Gianessi et al.
Addiction biology, 25(3), e12768-e12768 (2019-05-06)
Individuals with alcohol use disorder exhibit compulsive habitual behaviors that are thought to be, in part, a consequence of chronic and persistent use of alcohol. The endocannabinoid system plays a critical role in habit learning and in ethanol self-administration, but
Jenny L Wilkerson et al.
The Journal of pharmacology and experimental therapeutics, 363(3), 394-401 (2017-10-04)
Diacylglycerol lipase (DAGL) α and β, the major biosynthetic enzymes of the endogenous cannabinoid (endocannabinoid) 2-arachidonylglycerol (2-AG), are highly expressed in the nervous system and immune system, respectively. Genetic deletion or pharmacological inhibition of DAGL-β protects against lipopolysaccharide (LPS)-induced inflammatory

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