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KT-109

Chemical Structure : KT-109

CAS No.: 1402612-55-8

KT-109 (KT109)

Catalog No.: PC-61838Not For Human Use, Lab Use Only.

KT-109 is a potent, selective inhibitor of DAGLβ with IC50 of 42 nM, displays about 60-fold selectivity over DAGLα.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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).

Physicochemical Properties

M.Wt 422.5
Formula C27H26N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

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.

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