| Identification | Back Directory | [Name]
KLH45 | [CAS]
1632236-44-2 | [Synonyms]
KLH45
KLH45 >=98% (HPLC)
N-Cyclohexyl-N-(2-phenylethyl)-4-[4-(trifluoromethoxy)phenyl]-2H-1,2,3-triazole-2-carboxamide | [Molecular Formula]
C24H25F3N4O2 | [MDL Number]
MFCD30742935 | [MOL File]
1632236-44-2.mol | [Molecular Weight]
458.48 |
| Chemical Properties | Back Directory | [Boiling point ]
561.0±60.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:30.0(Max Conc. mg/mL);65.43(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);65.43(Max Conc. mM) | [form ]
Solid-Liquid Mixture | [pka]
-1.76±0.20(Predicted) | [color ]
Off-white to light yellow | [InChIKey]
FYOYNRLSBYWAHL-UHFFFAOYSA-N | [SMILES]
O=C(N(CCC1=CC=CC=C1)C2CCCCC2)N(N=C3)N=C3C4=CC=C(OC(F)(F)F)C=C4 |
| Hazard Information | Back Directory | [Description]
KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM). It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 μM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 μM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid. | [Uses]
KLH45 is a novel selective inhibitor of DDHD2. | [in vivo]
KLH45 (20 mg/kg; administered every 12 h) for a total of 4 d exhibits significant elevations in several of the TAGs that accumulated in the brains of DDHD2?/? mice[1].
| Animal Model: | Mice[1].
| | Dosage: | 5-40 mg/kg. | | Administration: | IP, once. | | Result: | Did not show altered brain TAGs.
|
| [References]
[1] JORDON M INLOES. The hereditary spastic paraplegia-related enzyme DDHD2 is a principal brain triglyceride lipase.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 41: 14924-14929. DOI: 10.1073/pnas.1413706111
[2] JORDON M. INLOES, Benjamin F. Cravatt*. Functional Contribution of the Spastic Paraplegia-Related Triglyceride Hydrolase DDHD2 to the Formation and Content of Lipid Droplets[J]. Biochemistry Biochemistry, 2017, 57 5: 827-838. DOI: 10.1021/acs.biochem.7b01028 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
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