1402612-55-8
1402612-55-8 structure
- Name: KT-109
- Chemical Name: (2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone
- CAS Number: 1402612-55-8
- Molecular Formula: C27H26N4O
- Molecular Weight: 422.522
- Create Date: 2020-01-12 06:41:50
- Modify Date: 2024-01-13 11:05:19
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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).
| Name | (2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone |
|---|---|
| Synonyms |
(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]- |
| 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) |
| 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 |