Exendin Fragment 9-39

Names

[ Name ]:
Exendin Fragment 9-39

[Synonym ]:
Exendin 9-39
Exendin(9-39)amide
L-Serinamide, 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-isoleucyl-L-alp 
ha-glutamyl-L-tryptophyl-L-leucyl-L-lysyl-L-asparaginylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-
UNII-5313W10MYT
Exendin-3 (9-39) amide
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-isoleucyl-L-α-glutamyl-L- tryptophyl-L-leucyl-L-lysyl-L-asparaginylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide
Exendin 3 (heloderma horridum),1-de-L-histidine-2-de-L-serine-3-de-L-aspartic acid-4-deglycine-5-de-L-threonine-6-de-L-phenylalanine-7-de-L-threonine-8-de-L-serine
MFCD00283195

Biological Activity

[Description]:

Exendin (9-39) is a specific and competitive glucagon-like peptide-1 receptor antagonist.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Glucagon Receptor

Peptides

Research Areas >> Metabolic Disease

[In Vitro]

GLP-1 plays a role in the control of fasting glucose. Exendin-(9-39), a truncated form of the GLP-1 agonist exendin-4, is a specific GLP-1 receptor antagonist in mice and humans. Exendin (9-39) significantly inhibits amino acid-stimulated insulin secretion in pancreatic islets isolated from neonates with KATPHI[1].

[In Vivo]

Insulin-to-glucose ratios are significantly lower during Exendin (9-39) infusion compared with vehicle[1]. Continuous subcutaneous infusion of exendin-(9-39) significantly raises fasting blood glucose levels in SUR-1 −/− mice without affecting glucose tolerance or insulin sensitivity[2].

[Animal admin]

Mice: Alzet miniosmotic pumps are implanted subcutaneously to deliver exendin (9-39) at a rate of 150 pmol/kg/min or vehicle (0.9% NaCl, 1% bovine serum albumin) for 2 weeks[2].

[References]

[1]. Calabria AC, et al. GLP-1 receptor antagonist exendin-(9-39) elevates fasting blood glucose levels in congenital hyperinsulinism owing to inactivating mutations in the ATP-sensitive K+ channel. Diabetes. 2012 Oct;61(10):2585-91.

[2]. De León DD, et al. Exendin-(9-39) corrects fasting hypoglycemia in SUR-1-/- mice by lowering cAMP in pancreatic beta-cells and inhibiting insulin secretion. J Biol Chem. 2008 Sep 19;283(38):25786-93.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₄₉H₂₃₄N₄₀O₄₇S

[ Molecular Weight ]:
3369.757

[ Exact Mass ]:
3367.687012

[ PSA ]:
1415.58000

[ LogP ]:
-5.88

[ Index of Refraction ]:
1.671

[ Storage condition ]:
-20°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
F+

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Hindbrain oxytocin receptors contribute to the effects of circulating oxytocin on food intake in male rats.

Endocrinology 155(8) , 2845-57, (2014)

Oxytocin (OT)-elicited hypophagia has been linked to neural activity in the nucleus of the solitary tract (NTS). Because plasma OT levels increase after a meal, we hypothesized that circulating OT act...

Endogenous glucagon-like peptide-1 reduces drinking behavior and is differentially engaged by water and food intakes in rats.

J. Neurosci. 34(49) , 16417-23, (2014)

Glucagon-like peptide-1 (GLP-1) is produced in the ileum and the nucleus of the solitary tract. It is well known that GLP-1 controls food intake, but there is a growing literature indicating that GLP-...

GLP-1 receptor activation modulates appetite- and reward-related brain areas in humans.

Diabetes 63(12) , 4186-96, (2014)

Gut-derived hormones, such as GLP-1, have been proposed to relay information to the brain to regulate appetite. GLP-1 receptor agonists, currently used for the treatment of type 2 diabetes (T2DM), imp...

Related Compounds

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