KT-109
KT-109 structure
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Common Name | KT-109 | ||
|---|---|---|---|---|
| CAS Number | 1402612-55-8 | Molecular Weight | 422.522 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 637.3±53.0 °C at 760 mmHg | |
| Molecular Formula | C27H26N4O | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 339.3±30.9 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of KT-109KT-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). |
| Name | (2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone |
|---|---|
| Synonym | More Synonyms |
| 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). |
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| 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) |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 637.3±53.0 °C at 760 mmHg |
| Molecular Formula | C27H26N4O |
| Molecular Weight | 422.522 |
| Flash Point | 339.3±30.9 °C |
| Exact Mass | 422.210663 |
| LogP | 5.23 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.653 |
| Storage condition | 2-8°C |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302-H413 |
| Precautionary Statements | P301 + P312 + P330 |
| Hazard Codes | Xn |
| RIDADR | NONH for all modes of transport |
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DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.
Nat. Chem. Biol. 8(12) , 999-1007, (2012) The endocannabinoid 2-arachidonoylglycerol (2-AG) is biosynthesized by diacylglycerol lipases DAGLα and DAGLβ. Chemical probes to perturb DAGLs are needed to characterize endocannabinoid function in b... |
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Development and optimization of piperidyl-1,2,3-triazole ureas as selective chemical probes of endocannabinoid biosynthesis.
J. Med. Chem. 56(21) , 8257-69, (2013) We have previously shown that 1,2,3-triazole ureas (1,2,3-TUs) act as versatile class of irreversible serine hydrolase inhibitors that can be tuned to create selective probes for diverse members of th... |
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Serine hydrolase inhibitors block necrotic cell death by preventing calcium overload of the mitochondria and permeability transition pore formation.
J. Biol. Chem. 289(3) , 1491-504, (2014) Perturbation of calcium signaling that occurs during cell injury and disease, promotes cell death. In mouse lung fibroblasts A23187 triggered mitochondrial permeability transition pore (MPTP) formatio... |
| (2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone |
| Methanone, (4-[1,1'-biphenyl]-4-yl-1H-1,2,3-triazol-1-yl)[2-(phenylmethyl)-1-piperidinyl]- |