Cas No.: | 1402612-55-8 |
Chemical Name: | Methanone, (4-[1,1-biphenyl]-4-yl-1h-1,2,3-triazol-1-yl)[2-(phenylmethyl)-1-piperidinyl]- |
Synonyms: | Methanone, (4-[1,1-biphenyl]-4-yl-1h-1,2,3-triazol-1-yl)[2-(phenylmethyl)-1-piperidinyl]- |
SMILES: | C1(C2C=CC=CC=2)C=CC(C2N=NN(C(N3CCCCC3CC3C=CC=CC=3)=O)C=2)=CC=1 |
Formula: | C27H26N4O |
M.Wt: | 422.521545886993 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | KT-109 is a potent, selective inhibitor of DAGLβ with IC50 of 42 nM, displays about 60-fold selectivity over DAGLα; shows negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL and ABHD11; disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids in mouse peritoneal macrophages; reverses nociceptive behaviour in mouse models of inflammatory and neuropathic pain; possesses one remaining off-target ABHD6 (IC50=16 nM). |
References: | References 1. Hsu KL, et al. Nat Chem Biol. 2012 Dec;8(12):999-1007. 2. Wilkerson JL, et al. Br J Pharmacol. 2016 May;173(10):1678-92. 3. Shin M, et al. Mol Pharm. 2017 Sep 13. doi: 10.1021/acs.molpharmaceut.7b00657. View Related Products by Target Diacylglycerol Lipase (DAGL) |