| Identification | Back Directory | [Name]
LCQ-908 | [CAS]
956136-95-1 | [Synonyms]
LCQ-908
LCQ 908NXA
Pradigastat
LCQ-908, >=98%
2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic Acid
trans-4-[4-[5-[[6-(Trifluoromethyl)-3-pyridinyl]amino]-2-pyridinyl]phenyl]cyclohexaneacetic acid
Cyclohexaneacetic acid, 4-[4-[5-[[6-(trifluoromethyl)-3-pyridinyl]amino]-2-pyridinyl]phenyl]-,trans- | [Molecular Formula]
C25H24F3N3O2 | [MDL Number]
MFCD25562905 | [MOL File]
956136-95-1.mol | [Molecular Weight]
455.47 |
| Chemical Properties | Back Directory | [Boiling point ]
611.0±55.0 °C(Predicted) | [density ]
1.286±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
4.72±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 μM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 μM, 1.66μM, 3.34μM and 0.973μM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro[1][2][3][4]. | [Biological Activity]
lcq908 is a diacylglycerol acyltransferase-1 (dgat-1) inhibitor. dgat-1 has been recognized to catalyze the final committed step of processing dietary fatty acids into triglycerides carried on chylomicrons for transport around the body. thus,inhibition of dgat-1 represents a novel approach to treat metabolic disease. | [in vitro]
in vitro studies suggest that glucuronidation is the predominant metabolism pathway for elimination of lcq908 in humans. lcq908 inhibited bcrp-mediated efflux activity in a dose-dependent fashion with an ic50 value of 5 μm. lcq908 also inhibited oatp1b1, oatp1b3, and oat3 activity in a concentration-dependent manner with estimated ic50 values of 1.66 ± 0.95 μm, 3.34 ± 0.64 μm, and 0.973 ± 0.11 μm, respectively [1]. | [in vivo]
lcq908 was fond to suppress the postprandial triglyceride levels in rats, dogs as well as monkeys. in rats whose lpl activity had been abolished, lcq908 reduced the postprandial accumulation of plasma triglyceride. additional, lcq908 decreased the postprandial rate of cm-tg secretion into the lymphatic duct and reduced the size of cms [2]. | [IC 50]
5 μm for bcrp-mediated efflux activity | [References]
[1] kulmatycki k,hanna i,meyers d,salunke a,movva a,majumdar t,natrillo a,vapurcuyan a,rebello s,sunkara g,chen jevaluation of a potential transporter-mediated drug interaction between rosuvastatin and pradigastat, a novel dgat-1 inhibitor. int j clin pharmacol ther.2015 may;53(5):345-55.
[2] meyers cd, serrano-wu m, amer a, chen j, eric r, commerford r, et al. the dgat1 inhibitor pradigastat decreases chylomicron secretion and prevents postprandial triglyceride elevation in humans [abstract]j clin lipidol.2013;7:285.
[3] charles meyers, daniel gaudet, karine tremblay, ahmed amer, jin chen, feng aimin. the dgat1 inhibitor lcq908 decreases triglyceride levels in patients with the familial chylomicronemia syndrome. journal of clinical lipidology, vol 6, no 3, june 2012, 266-267. |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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