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LUF 6283

Names

[ CAS No. ]:
92933-48-7

[ Name ]:
LUF 6283

[Synonym ]:
5-butyl-[1,3,5]triazinane-2-thione
Dihydrokainic acid
5-Butyl-1(2)H-pyrazol-3-carbonsaeure
5-Butyl-tetrahydro-s-triazin-2(1H)-thion
5-butyl-1,4,5,6-tetrahydro-1,3,5-triazine-2-thiol
1-Butyl-hexahydrotriazinthion-4
5-butyl-1(2)H-pyrazole-3-carboxylic acid

Biological Activity

[Description]:

LUF6283 is a potent and orally active HCA(2) partial agonist, with a Ki of 0.55 µM. LUF6283 can achieve the beneficial lipid lowering effect of niacin without producing the unwanted cutaneous flushing side effect[1].

[Related Catalog]:

Research Areas >> Metabolic Disease
Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

[Target]

EC50: 0.32 ± 0.06 μM (pERK1/2)[1]


[In Vivo]

LUF6283 (C57BL/6 mice, 400 mg/kg, Oral gavage, once a day for 4 weeks) has no effect on adipose tissue ATGL/HSL expression, and significantly reduces the expression of apolipoprotein B (APOB)[1].

[References]

[1]. Li Z, et al. Effects of pyrazole partial agonists on HCA(2) -mediated flushing and VLDL-triglyceride levels in mice. Br J Pharmacol. 2012 Oct;167(4):818-25.

Chemical & Physical Properties

[ Molecular Formula ]:
C8H12N2O2

[ Molecular Weight ]:
168.19300

[ Exact Mass ]:
168.09000

[ PSA ]:
65.98000

[ LogP ]:
1.45050

MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route


Related Compounds