Cotadutide-acetate-MEDI0382-acetate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECotadutide acetateCat. No.: HY-P2231ASynonyms: MEDI0382 acetate分式: CHNO分量: 3788.14Sequence: 1-palmtoyl-G; HisSerGlnGlyThrPheThrSerAspLysSerGluTyrLeuAspSerGluArgAlaArgAspP heValAlaTrpLeuGluAlaGlyGly-(Amide bridge: Ggu 1-Lys10)Seq

2、uence Shortening:1-palmtoyl-G;HSQGTFTSDKSEYLDSERARDFVAWLEAGG(Amide bridge:Ggu1-Lys10)作靶点: Glucagon Receptor作通路: GPCR/G Protein储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Cotadutide acetate (MEDI0382 acetate)胰糖素样肽-1 (GLP-1) 和胰糖素受体 (glucagon receptor

3、)的有效双重 肽激动剂，EC50 值分别为 6.9 pM 和 10.2 pM。Cotadutide acetate (MEDI0382 acetate) 有促进减肥和控制糖的能，有潜于肥胖症和 2 型糖尿病 (T2D) 的研究。IC50 & Target EC50: 6.9 pM (GLP-1); 10.2 pM (glucagon receptor) 1体外研究Cotadutide acetate (MEDI0382 acetate) shows EC50 values of 6.9 and 10.2pM as measured by cAMPgeneration in CHO cells

4、overexpressing hum an recom binant GLP1 or glucagon receptors in the presence of 0.1%BSA, which are within 10fold of the native ligands 1.Cotadutide acetate (MEDI0382 acetate) stim ulates aconcentrationdependent increase in cAMP accum ulation in rat (INS1 832/3) and hum an (EndoCH1) pancreatic cell

5、lines (EC50=226 pM,1051 pM, respectively), as well as rat, m ouse and hum an hepatocytes (462 pM, 840 pM,1447 pM, respectively) 1.Cotadutide acetate (MEDI0382 acetate) has relative potency against GLP1R and GCGRactivity in hum an, cynom olgus m onkey, m ouse and rat transfected GLP1 (GLP1R) or gluca

6、gon (GCGR) receptorsexpressed CHO cells, The EC50 values are 188 pM, 682 pM; 5.2pM, 318 pM; 74pM, 614 pM; and 50 pM, 24173 pM1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEfor Hum an, m onkey, m ouse and rat GLP1R and GCGR activities, respectively 1.体内研究 Cotadutide acetate (MEDI0382 acetate) (subc

7、utaneous injection; 10nmol/kg; once) robustly suppresses foodintake in DIO mice relative to vehicletreated controls during 012hours after adm inistration. Mean food intake isreduced during this tim e interval to approxim ately 31% of control m ice treated with vehicle. The effect of MEDI0382 isevide

8、nt early (02hours postdose), the term inal plasm a halflife of MEDI0382 in m ice after subcutaneousadm inistration is approxim ately 5hours 1.Cotadutide acetate (MEDI0382 acetate) (subcutaneous injection; 10 or 30nm ol/kg; once daily; 14-16 weeks) reduces body weight. reduced body weight.The m ean b

9、ody weight of vehicletreatedanim als increased by 2.5% of starting body weight over the course of the 4week study, whereas the m ean body weightloss is 21%, 30% of starting body weight at dose levels of 10nm ol/kg MEDI0382, 30nm ol/kg MEDI0382, respectively1.Animal Model: DIO mice 1Dosage: 10nmol/kg

10、Administration: Subcutaneous injectionResult: Showed a redction of food intake in mice after an acute administration.Animal Model: DIO mice 1Dosage: 10 or 30nmol/kgAdministration: Subcutaneous injectionResult: Reduced body weight and food intake and improves glucose tolerance in DIO mice.REFERENCES1. Henderson SJ,et al. Robust anti-obesity and metabolic effects of a dual GLP-1/glucagon receptor peptide agonist in rodents and non-human primates.Diabetes Obes Metab. 2016 Dec;18(12):1176-1190.McePdfHeightCaution: Product has not been