Exenatide acetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Exenatideacetate (Exendin-4acetate)是Exenatide的乙酸盐，是一种高效、长效的胰高血糖素样肽-1受体(GLP-1)激动剂，IC50为3.22nM。

Exenatide acetate (Exendin-4 acetate) is the acetate of Exenatide, which is highly potent, long-acting glucagon-like peptide-1 receptor (GLP-1) agonist with IC50 of 3.22 nM.Diabetes Phase 3 Clinical.

In human umbilical vein endothelial cells, Exendin-4 significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 μM at 48 hour.

Both low- and high-dose Exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose, and calculated HOMA scores compared with control. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period. Animals treated with Exendin-4 have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats. Exendin-4 treatment is associated with lower leptin levels as well as lower HOMA values in rats. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO.

Exendin-4 acetate

GPCR/G Protein

Glucagon Receptor

Glucagon Receptor

Metabolic Disease

Diabetes

914454-01-6

4246.624

C186H286N50O62S

>98% (HPLC)

DMSO

CCC(C)C(CNC(CCC(=O)O)CN[CH]CNC(CC(C)C)CNC(CCCCN)CNC(CC(=O)N)CNCCNCCN1CCCC1CNC(CNC(CNCCN[CH]CN2CCCC2CN3CCCC3CN4CCCC4CNC(CN)CO)CO)CO)NC[CH]NCC(CC(C)C)NC[CH]

L-Serinamide, L-histidylglycyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-leucyl-L-seryl-L-lysyl-L-glutaminyl-L-methionyl-L-α-glutamyl-L-α-glutamyl-L-α-glutamyl-L-alanyl-L-valyl-L-arginyl-L-leucyl-L-phenylalanyl-L-isole

(-20℃)

With Ice Pack

≥ 2 years