Exendin-4

Short Summary : GLP-1 activator

Category : GPCR/G protein|Glucagon Receptor

Purity : 0.9882

CAS Number : 141758-74-9

Formula : C184H282N50O60S

Molecular Weight : 4186.57

SMILE : CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCCC3C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)N6CCCC6C(=O)NC(CO)C(=O)N)NC(=O)C(CC7=CC=CC=C7)NC(=O)C(CC(C)C)NC(

Solubility : Soluble to 1 mg/ml in sterile water

Storage : Store at -20°C

Description : Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, mimics the activity of mammalian incretin hormone glucagon-like peptide 1 (GLP-1), and thus, promotes insulin secretion and functions in the control of glucose [1].In vitro: Exendin-4 showed a pronounced effect on intracellular cAMP generation. Treatment of GLP-1 in combination with exendin-4 showed additive action on the generation of cAMP. In isolated rat islets and in mouse insulinoma beta TC-1 cells, Exendin-4 stimulated the glucose-induced insulin secretion in a dose dependent manner [2]. In basal forebrain cholinergic neurons, exendin-4 greatly reduced ibotenic acid-induced depletion of choline acetyltransferase immunoreactivity [3].In vivo: In ob/ob mice, administration of Exendin-4 (10 g/kg or 20 g/kg) improved insulin sensitivity and significantly reduced serum glucose and hepatic steatosis. Exendin-4 appeared to effectively reverse hepatic steatosis in ob/ob mice by improving insulin sensitivity [1]. In athymic mice, 63% of exendin-4-treated mice achieved graft function compared with 21% of untreated mice (p = 0.033) in the short-term study. 88% of treated mice had functioning grafts compared with 22% of controls (p = 0.015) in the long-term study. Exendin-4-treated mice gained significantly more weight than the untreated counterparts [4].References:Ding X, Saxena N K, Lin S, et al. Exendin4, a glucagonlike protein1 (GLP1) receptor agonist, reverses hepatic steatosis in ob/ob mice[J]. Hepatology, 2006, 43(1): 173-181.Gke R, Fehmann H C, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells[J]. Journal of Biological Chemistry, 1993, 268(26): 19650-19655.Perry T A, Haughey N J, Mattson M P, et al. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4[J]. Journal of Pharmacology and Experimental Therapeutics, 2002, 302(3): 881-888.Sharma A, Srenby A, Wernerson A, et al. Exendin-4 treatment improves metabolic control after rat islet transplantation to athymic mice with streptozotocin-induced diabetes[J]. Diabetologia, 2006, 49(6): 1247-1253.

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