GLP-1(32-36)amide,一种衍生自糖调节激素 GLP-1 的 C 末端的五肽。GLP-1(32-36)amide 可抑制糖尿病小鼠的体重增加并调节全身葡萄糖代谢。
GLP-1(32-36)amide Chemical Structure
CAS No. : 1417302-71-6
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GLP-1(32-36)amide 相关产品
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生物活性
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice[1][2].
体外研究 (In Vitro)
GLP-1(32-36)amide (0.1-10 μM; 24 h) retains cell viability and decreases apoptosis against Streptozotocin (STZ; 1 μM) in INS‐1 cells[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
INS‐1 cells
Concentration:
0.1, 1, 10 μM
Incubation Time:
24 hours
Result:
Decreased cell viability only approximately 30% in 0.1 μM and approximately 20% in ≥1 μM while approximately 45% in saline-treated controls.
体内研究 (In Vivo)
GLP-1(32-36)amide (1 μmol/kg; i.p. once daily for 21 d) protects islet from damage, inhibits weight gain, and relieves symptoms of polydipsia in diabetic mice[2]. GLP-1(32-36)amide (1 μmol/kg; a single i.p.) slightly reduces the mean glucose lever at 30 min after the challenge of glucose in normal mice[2]. GLP-1(32-36)amide (50-70 nmol/kg/d; infusion for 12-16 weeks) prevents the development of diet-induced obesity and hepatic steatosis in high fat-fed mice[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male KM mice (6-8 weeks; 18-22 g) injected with STZ[2]
Dosage:
1 μmol/kg
Administration:
I.p. once daily for 21 days
Result:
Significantly lowered the cumulative values of food and water intake. Lowered fasting glucose. Reduced the level of Hemoglobin A1c (HbA1c). Improved glucose tolerance. Suppressed body weight gain.
分子量
570.73
Formula
C25H50N10O5
CAS 号
1417302-71-6
Sequence
Leu-Val-Lys-Gly-Arg-NH2
Sequence Shortening
LVKGR-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Elahi D, et, al. GLP-1(32-36)amide, a novel pentapeptide cleavage product of GLP-1, modulates whole body glucose metabolism in dogs. Peptides. 2014 Sep;59:20-4.
[2]. Sun L, et, al. Novel Pentapeptide GLP-1 (32-36) Amide Inhibits β-Cell Apoptosis In Vitro and Improves Glucose Disposal in Streptozotocin-Induced Diabetic Mice. Chem Biol Drug Des. 2015 Dec;86(6):1482-90.
[3]. Tomas E, et, al. GLP-1(32-36)amide Pentapeptide Increases Basal Energy Expenditure and Inhibits Weight Gain in Obese Mice. Diabetes. 2015 Jul;64(7):2409-19.
GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects[1].
体外研究 (In Vitro)
Different from DPP-IV, NEP, which cleaves GLP-1(7-36)amide or GLP-1(9-36)amide to generate GLP-1(28-36)amide, is widely distributed in endothelial cells, vascular smooth muscle cells, cardiac cells and renal epithelial cells[1]. GLP-1(28-36)amide (100 nM) treatment on hepatocytes for 24 hours directly modulates mitochondrial oxidative metabolism, such as gluconeogenesis in mitochondria of hepatocytes[1]. The plasma half-life of GLP-1(28-36)amide is longer in human hepatocytes (t1/2 = 24 min) than that in mouse hepatocytes (t1/2 = 13 min)[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
The administration of GLP-1(28-36)amide at a rate of 18.5 nmol/kg BW/day for 9 weeks to diet-induced obese mice diminishes the development of hepatic steatosis[1]. The intraperitoneal injection of 18 nmol/kg GLP-1(28-36)amide once daily for 9 weeks show cytoprotective effect on pancreatic β cells by increasing mass and promoting proliferation in a β-cell injury diabetic mouse model[1]. An in vivo study in high-fat diet-fed mice indicates that a six-week administration of 18.5 nmol/kg GLP-1(28-36)amide improved hepatic glucose disposal, which is associated with increased cAMP levels and phosphorylation of PKA target[1]. Administered GLP-1(28-36)amide for 20 min to male C57BL6/J mice (10-12 week old), then isolated hearts underwent 30 min of global ischemia and 40 min of reperfusion, the recovery of left ventricular developed pressure (LVDP) is significantly greater in GLP-1(28-36)amide group compared to vehicle-treated hearts[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1088.35
Formula
C54H85N15O9
CAS 号
1225021-13-5
Sequence
Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH2
Sequence Shortening
FIAWLVKGR-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
HAEGTFTSD is a 9-residue peptide of human GLP-1 peptide or GLP-1(7-36), amide (HY-P0054A). GLP-1(7-36), amide is a physiological incretin hormone that stimulates insulin secretionin a glucose-dependant manner[1]
体外研究 (In Vitro)
The GLP-1 (7-36) amide is a product of the preproglucagon gene, which is secreted from intestinal L-cells, in response to the ingestion of food. GLP-1 exerts multiple actions by stimulating insulin secretion from pancreatic β-cells, in a glucose dependent manner (insulinotropic action). GLP-1 lowers circulating plasma glucagon concentration, by inhibiting its secretion (production) from α-cells. GLP-1 also exhibits properties like stimulation of β-cell growth, appetite suppression, delays gastric emptying and stimulation of insulin sensitivity[1]. The peptide analogs of GLP-1 are useful as glucagon-like peptide 1 receptor agonists[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
963.94
Formula
C40H57N11O17
CAS 号
926018-45-3
Sequence Shortening
HAEGTFTSD
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. K Hupe-Sodmann, et al. Characterisation of the processing by human neutral endopeptidase 24.11 of GLP-1(7-36) amide and comparison of the substrate specificity of the enzyme for other glucagon-like peptides. Regul Pept. 1995 Aug 22;58(3):149-56.