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Exendin-4

Catalog No. T3967 CAS 141758-74-9

Synonyms: Exenatide, Exenatide Acetate

Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.

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Exendin-4, CAS 141758-74-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 57.00
2 mg	In stock	$ 83.00
5 mg	In stock	$ 137.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 443.00
100 mg	In stock	$ 639.00

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Purity: 99.72%

Purity: 97.84%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.
Targets&IC50	GLP1:3.22 nM
In vitro	In HUVECs, exendin-4 dose-dependently significantly increases NO production, eNOS phosphorylation and GTPCH1 level[2]. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells (IC50 5 μM) at 48 hours [3].
In vivo	In ob/ob mice, the treatment of exendin-4 improve serum ALT and reduce serum glucose, insulin levels and calculated HOMA scores compared with control. In the final 4 weeks of the study period, exendin-4-treated ob/ob mice sustain an obvious reduction in the net weight gain[4]. Animals treated with exendin-4 have more pyknotic nuclei, more pancreatic acinar inflammation and weigh significantly less than control rats[5]. Exenatide leads to dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by CO and NO[6].

Synonyms	Exenatide, Exenatide Acetate
Molecular Weight	4186.57
Formula	C184H282N50O60S
CAS No.	141758-74-9

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

H2O: 1.23 mg/mL), Sonication and heating are recommended.

References and Literature

1. Doyle ME, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity. Regul Pept. 2003 Jul 15;114(2-3):153-8. 2. Wei R, et al. Exenatide exerts direct protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner. Am J Physiol Endocrinol Metab. 2016 Jun 1; 310(11):E947-57. 3. Ding X, et al. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/obmice. Hepatology. 2006 Jan;43(1):173-81. 4. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9. 5. Sélley, E., Kun, S., Szijártó, I., Laczy, B., Kovács, T., & Fülöp, F. et al. (2014). Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production. Cardiovascular Diabetology, 13(1), 69. doi: 10.1186/1475-2840-13-69 6. Fidan-YaylalI G, et al. Antidiabetic exendin-4 activates apoptotic pathway and inhibits growth of breast cancer cells. Tumour Biol. 2016 Feb;37(2):2647-53. 7. Huang L, Ma R, Lin T, et al. Glucagon-like peptide-1 receptor pathway inhibits extracellular matrix production by mesangial cells through store-operated Ca2+ channel[J]. Experimental Biology and Medicine. 2019: 1535370219876531.

Citations

1. Huang L, Ma R, Lin T, et al. Glucagon-like peptide-1 receptor pathway inhibits extracellular matrix production by mesangial cells through store-operated Ca2+ channel. Experimental Biology and Medicine. 2019: 1535370219876531. 2. Ren W, Chen J, Wang W, et al.Sympathetic nerve-enteroendocrine L cell communication modulates GLP-1 release, brain glucose utilization, and cognitive function.Neuron.2024

Related compound libraries

This product is contained In the following compound libraries：

NO PAINS Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets

LGD-6972 GLP-1R Antagonist 1 Glucagon (1-29), bovine, human, porcine hydrochloride PF-06882961 Tris GLP-1R modulator C5 Lixisenatide acetate (320367-13-3 free base) Exendin-4 acetate LSN3318839

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Keywords

Exendin-4 141758-74-9 GPCR/G Protein Glucagon Receptor inhibit GCGR Inhibitor Exenatide Exenatide Acetate Exendin 4 Exendin4 inhibitor

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