JZL 184

JZL 184 구조식 이미지
카스 번호:
1101854-58-3
상품명:
JZL 184
동의어(영문):
CS-815;CS-1861;JZL 184;JZL-184; JZL 184;JZL 184 JZL184 JZL-184;JZL184 (with 15% inorganics);MAGL Inhibitor III, JZL184 - CAS 1101854-58-3 - Calbiochem;4-Nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)(hydroxy)Methyl]-1-piperidinecarboxylate;4-Nitrophenyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate;4-[Bis(1,3-benzodioxol-5-yl)hydroxymethyl]-1-piperidinecarboxylic acid 4-nitrophenyl ester
CBNumber:
CB12535677
분자식:
C27H24N2O9
포뮬러 무게:
520.49
MOL 파일:
1101854-58-3.mol
MSDS 파일:
SDS

JZL 184 속성

녹는점
116-120°C
끓는 점
706.4±60.0 °C(Predicted)
밀도
1.467±0.06 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO에 용해됩니다(최대 25mg/ml).
물리적 상태
흰색에서 회백색 고체
산도 계수 (pKa)
13.32±0.29(Predicted)
색상
연한 노란색에서 황록색까지
안정성
-20°C에서 DMSO에 최대 2개월 동안 보관 가능
CAS 데이터베이스
1101854-58-3
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
유엔번호(UN No.) UN 2811 6.1 / PGIII
HS 번호 29349990
그림문자(GHS): GHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
예방조치문구:
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

JZL 184 C화학적 특성, 용도, 생산

개요

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA) 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. JZL 184 is a potent and selective inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 8 nM and 4 μM for inhibition of MAGL and fatty acid amide hydrolase in mouse brain membranes, respectively. 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.

용도

JZL 184 hydrate has been used as an inhibitor of monoacylglycerol lipase to study its effect on human osteoblast differentiation and proliferation and postsynaptic neurons.

Biochem/physiol Actions

JZL184 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, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.

JZL 184 준비 용품 및 원자재

원자재

준비 용품


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