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Exendin-4 (acetate)

Item № 11096
CAS № 914454-01-6
Purity ≥95%
product image
                (CAS 914454-01-6)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     500 µg $85.00 0.00
     1 mg $153.00 0.00
     5 mg $680.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

Description
Synonyms
  • Exenatide Acetate

Exendin-4 is a potent peptide agonist of the glucagon-like peptide 1 (GLP-1) receptor (Ki = 136 pM).1,2,3,4 By activating the GLP-1 receptor, it stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes.2 Exendin-4 was first isolated from the venom of H. horridum and consequently synthesized, with the recombinant peptide referred to as ‘exenatide.’ Exenatide protects hippocampal neurons against glutamate-induced apoptosis, suggesting utility in neuropathies associated with type 2 diabetes and in neurodegenerative diseases.5,6 Exenatide also has anxiolytic and anti-depressant effects and induces satiety.6,7

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Technical Information
CAS Number
914454-01-6
Synonyms
  • Exenatide Acetate
Molecular Formula
C184H282N50O60S • C2H4O2
Formula Weight
4246.6
Purity
≥95%
Formulation
A crystalline solid
SMILES
NC([C@H](CO)NC([C@@H]1CCCN1C([C@@H]2CCCN2C([C@@H]3CCCN3C([C@@H](NC(CNC([C@H](CO)NC([C@H](CO)NC([C@@H]4CCCN4C(CNC(CNC([C@H](CC(N)=O)NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@@H](NC([C@H](CCC(O)=O)NC([C@@]([C@H](CC)C)([H])NC([C@@H](NC([C@H](CC(C)C)NC([C@H](
InChI Code
InChI=1S/C184H282N50O60S.C2H4O2/c1-16-94(10)147(178(289)213-114(52-58-144(257)258)163(274)218-121(73-101-77-195-105-39-24-23-38-103(101)105)168(279)215-116(68-90(2)3)165(276)205-107(41-26-28-61-186)158(269)219-122(75-134(189)243)154(265)198-79-135(24
InChI Key
YEAXWAGAAYUUBX-JVTOQCAZSA-N
Origin
  • Animal/Rabbit

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Eng, J., Kleinman, W.A., Singh, L., et al. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas The Journal of Biological Chemisty 267(11), 7402-7405 (1992).

2. Göke, 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 β-cells The Journal of Biological Chemisty 268(26), 19650-19655 (1993).

3. Thorens, B., Porret, A., Bühler, L., et al. Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor Diabetes 42(11), 1678-1682 (1993).

4. Donnelly, D. The structure and function of the glucagon-like peptide-1 receptor and its ligands British Journal of Pharmacology 166(1), 27-41 (2012).

5. Perry, T., Haughey, N.J., Mattson, M.P., et al. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4 Journal of Pharmacology and Experimental Therapeutics 302(3), 881-888 (2002).

6. Komsuoglu Celikyurt, I., Mutlu, O., Ulak, G., et al. Exenatide treatment exerts anxiolytic- and antidepressant-like effects and reverses neuropathy in a mouse model of type-2 diabetes Med.Sci.Monit.Basic Res. 20, 112-117 (2014).

7. van Bloemendaal, L., Ten Kulve, J.S., la Fleur, S.E., et al. Effects of glucagon-like peptide 1 on appetite and body weight: Focus on the CNS Journal of Endocrinology 221(7), T1-T16 (2014).

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