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KT172

产品编号:4086220
规格:≥98% (HPLC)
CAS NO:1402612-56-9
包装规格:5 MG,25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
40862205 MG1530
408622025 MG4490
产品别名

1402612-56-9

KT172

[4-(2′-Methoxy[1,1′-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylmethyl)-1-piperidinyl]-methanone

Cravatt Reagent

(2-Benzylpiperidin-1-yl)(4-(2′-methoxy-[1,1′-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)methanone

结构式
基本信息
Empirical Formula【经验(实验)分子式】
C28H28N4O2
Molecular weight
452.55
MDL number
MFCD26960820
PubChem Substance ID【PubChem化学物质编号】
329826017
NACRES
NA.77
Biochem/physiol Actions【生化/生理作用】
KT172 is a Diacylglycerol lipase (DAGL) inhibitor selective for DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT172 is a new potent and selective DAGLβ inhibitor with an IC50 of 60 nM for recombinant DAGLβ vs 140 nM for DAGLα, although it is not active against DAGLα in vivo, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling or against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 values of 5 nM) can be controlled for by use of the related compounds, KT195 SML1308 or KT185 SML1249, potent and selective ABDH6 inhibitors with negligible activity against DAGLβ. KT172 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
powder
color【颜色】
white to beige
solubility【溶解性】
DMSO: 20 mg/mL, clear
storage temp.【储存温度】
2-8℃
SMILES string
O=C(N1N=NC(C2=CC=C(C3=C(OC)C=CC=C3)C=C2)=C1)N4CCCCC4CC5=CC=CC=C5
InChI
1S/C28H28N4O2/c1-34-27-13-6-5-12-25(27)22-14-16-23(17-15-22)26-20-32(30-29-26)28(33)31-18-8-7-11-24(31)19-21-9-3-2-4-10-21/h2-6,9-10,12-17,20,24H,7-8,11,18-19H2,1H3
InChI key
MXVVJNJNDCJCFS-UHFFFAOYSA-N
packaging【包装】
5, 25 mg in glass bottle
安全信息
Storage Class Code【储存分类代码】
13 - Non Combustible Solids
WGK
WGK 3
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