LCQ-908
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:对BCRP介导的流出活性IC50为5 μM。
LCQ908是一种二酰基甘油酰基转移酶-1(DGAT-1)抑制剂。已知DGAT-1催化乳糜微粒上进行的将膳食脂肪酸加工为甘油三酯以全身转运的最后关键步骤。因此,抑制DGAT-1代表了治疗代谢性疾病的一种新方法。
体外:体外研究表明,葡萄糖醛酸化是人类中LCQ908消除的主要代谢途径。 LCQ908剂量依赖性地抑制BCRP介导的流出活性,IC50值为5 μM。 LCQ908还浓度依赖性地抑制OATP1B1、OATP1B3和OAT3活性, 估计的IC50值分别为1.66±0.95 μM、3.34±0.64 μM和0.973±0.11 μM [1]。
体内:LCQ908抑制大鼠、狗以及猴子餐后甘油三酯水平。在移除LPL活性的大鼠中,LCQ908降低血浆甘油三酯的餐后累积。另外,LCQ908 降低餐后CM-TG分泌进入淋巴管的比率并减小CMs的体积[2]。
临床试验:在临床试验中,LCQ908能够降低维持低脂肪饮食的家族性乳糜微粒血症综合征患者的空腹甘油三酯水平,并代表治疗这种罕见疾病的一种潜在疗法[3]。
参考文献:
[1] Kulmatycki K,Hanna I,μMeyers D,Salunke A,μMovva A,μMajumdar 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.
Storage | Store at -20°C |
M.Wt | 455.47 |
Cas No. | 956136-95-1 |
Formula | C25H24F3N3O2 |
Synonyms | Pradigastat;LCQ908;LCQ 908 |
Solubility | Soluble in DMSO |
Chemical Name | 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid |
SDF | Download SDF |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |