| LCQ-908DGAT1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 956136-95-1 | SDF | Download SDF |
| Synonyms | Pradigastat;LCQ908;LCQ 908 | ||
| Chemical Name | 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid | ||
| Canonical SMILES | C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=NC=C(C=C3)NC4=CN=C(C=C4)C(F)(F)F | ||
| Formula | C25H24F3N3O2 | M.Wt | 455.47 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 5 μM for BCRP-mediated efflux 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].
Clinical trial: In a clinical trial, LCQ908 was found to be able to lower fasting triglyceride levels in familial chylomicronemia syndrome patients maintained on a very low-fat diet, and represents a potential drug treatment for this orphan disease [3].
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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看有关产前诊断的一个资料，提到：“凡是酶活性能在成纤维细胞中表达均可用绒毛或羊水细胞的酶活性测定进行产前诊断，如溶酶体贮积症。”
不太理解，为什么成纤维细胞中表达的酶就能在绒毛或羊水细胞中测出来呢？绒毛的细胞跟成纤维细胞没什么直接关系吧？或者是因为成纤维细胞脱落到羊水中，破裂，然后就可以检测了？
求各位解答，谢谢。
如癌症的CA抗原系列、用于测胆汁酸、尿酸之类的酶。
转换酶中的一类。催化氨基酸和a-氧代酸（a-酮酸
)或醛酸之间的氨基转换反应，生成与原来的a-氧代酸或醛酸相应的a-氨基酸或ω-
氨基酸，原来氨基酸转变成相应的氧代酸。转氨酶催化的反应都是可逆的。转氨酶可按底物的不同分成3大类。L-a-氨基酸（酮酸转氨酶） 、ω-
氨基酸（酮酸转氨酶）和D-氨基酸转氨酶。转氨酶的辅基是磷酸吡哆醛或磷酸吡哆胺，两者在转氨基反应中可互相变换。
转氨酶参与氨基酸的分解和合成。氨基酸转氨后生成的酮酸或醛酸可经氧化分解而供能，也可转变成糖类或脂肪酸。相反，酮酸或醛酸也可经转氨酶的作用而生成非必需氨基酸。某些氨基酸之间的互变也有转氨酶参与。在高等动物各组织中，活力最高的转氨酶是谷氨酸
： 草酰乙酸转氨酶（ GOT ）和谷氨酸：丙酮酸转氨酶（GPT）。
转氨酶是人体代谢过程中必不可少的“催化剂”，主要存在于肝细胞内。当肝细胞发生炎症、坏死、中毒等，造成肝细胞受损时，转氨酶便会释放到血液里，使血清转氨酶升高。
通常，体检中主要检查的转氨酶有丙氨酸转氨酶（ALT，俗称谷丙转氨酶）和天门冬氨酸转氨酶（AST，俗称谷草转氨酶），其中尤以前者（ALT）最为常用。1%的肝脏细胞损害，可以使血中ALT的浓度增加1倍。因此，ALT水平可以比较敏感地监测到肝脏是否受到损害。
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