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艾塞那肽

艾塞那肽用途

Exendin (9-39) 是特异竞争性的 glucagon-like peptide-1 受体拮抗剂。

艾塞那肽名称

[ CAS 号 ]:
133514-43-9

[ 中文名 ]:
艾塞那肽

[ 英文名 ]:
Exendin Fragment 9-39

[英文别名 ]:

Exendin 9-39
Exendin(9-39)amide
UNII-5313W10MYT
Exendin-3 (9-39) amide
MFCD00283195

艾塞那肽生物活性

[ 描述 ]:

Exendin (9-39) 是特异竞争性的 glucagon-like peptide-1 受体拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 胰高血糖素受体

多肽产品

研究领域 >> 代谢疾病

[体外研究]

GLP-1在控制空腹血糖中起作用。 Exendin-(9-39)是GLP-1激动剂exendin-4的截短形式,是小鼠和人的特异性GLP-1受体拮抗剂。 Exendin(9-39)显着抑制从KATPHI新生儿分离的胰岛中氨基酸刺激的胰岛素分泌[1]。

[体内研究]

与载体相比,Exendin(9-39)输注期间胰岛素与葡萄糖的比率显着降低[1]。连续皮下输注exendin-(9-39)可显着提高SUR-1 -/-小鼠的空腹血糖水平,而不影响葡萄糖耐量或胰岛素敏感性[2]。

[动物实验]

小鼠：将Alzet miniosmotic泵皮下植入以150pmol / kg / min的速率递送exendin（9-39）或载体（0.9％NaCl，1％牛血清白蛋白）2周[2]。

[参考文献]

[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.

[相关活性小分子]

艾塞那肽物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 分子式 ]:
C₁₄₉H₂₃₄N₄₀O₄₇S

[ 分子量 ]:
3369.757

[ 精确质量 ]:
3367.687012

[ PSA ]:
1415.58000

[ LogP ]:
-5.88

[ 折射率 ]:
1.671

[ 储存条件 ]:
-20°C

艾塞那肽安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
F+

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

艾塞那肽文献

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...

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