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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Lixisenatide is a synthetic, potent and selective GLP-1 receptor agonist with Ki value of 1.33nM. It is used in the treatment for type 2 diabetes mellitus (T2DM) and suggests actions that are highly relevant to the long-term maintenance of glucose homeostasis. Lixisenatide is a 44 amino acid peptide and shares similar sequence with pharmacologically active forms of human GLP-1 or exendin-4. ZP10A demonstrated dose-dependent improvement of glucose tolerance with an ED50 value of 0.02 nmol/kg i.p. in an oral glucose tolerance test (OGTT) in diabetic db/db mice. Long-term stimulation by Lixisenatide at 10nM for 24h led increased level of Akt-phosphorylation in INS-1 cells. Lixisenatide at 10nM protected rat-derived β-cell line, Ins-1 cells, from both lipid- and cytokine-induced apoptosis. Also it prevented lipotoxicity-induced insulin depletion in human islets and preserved insulin production, storage and pancreatic β-cell function in vitro. Lixisenatide improved basal blood glucose and HbA1c with a rapid onset and sustained duration of action, and prevented the deterioration of pancreatic responsiveness and glucose homeostasis in animal models of diabetes. It delayed gastric emptying and reduced food intake.
作用机制
Lixisenatide is a GLP-1 analogue.
Lixisenatide/利西拉来 细胞实验
Cell Line
Concentration
Treated Time
Description
References
INS-1832/3 cells
100 nM
16-18 hours
Measure insulin secretion, results showed reduced maximal insulin release with Lixisenatide compared to exendin-4
Br J Pharmacol. 2020 Sep;177(17):3905-3923
CHO-K1-SNAP-GLP-1 receptor cells
100 nM
30 minutes
Measure GLP-1 receptor recycling, results showed slower recycling after Lixisenatide treatment compared to exendin-4
Br J Pharmacol. 2020 Sep;177(17):3905-3923
C. elegans
6 µM, 2 µM, 0.6 µM, 0.2 µM, 0.02 µM
12 days
To evaluate the antioxidative properties of Lixisenatide under high glucose conditions in C. elegans. Results showed that Lixisenatide significantly reduced ROS formation under HG conditions, independent of concentration.
Acta Diabetol. 2023 Nov;60(11):1551-1565
Rat cardiomyocytes
100 nM
18 hours
Lixisenatide reduced cardiomyocyte apoptosis and increased fractional shortening.
J Transl Med. 2013 Mar 28;11:84
Lixisenatide/利西拉来 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
STZ-induced diabetic model
Subcutaneous injection
150 µg/kg body weight
5 days a week for 12 weeks
To assess the protective effects of Lixisenatide on diabetic retinopathy. Results showed that Lixisenatide significantly reduced the number of acellular capillaries, preserved retinal vasculature and neuroretinal function, and mitigated macro- and microglial activation.
Acta Diabetol. 2023 Nov;60(11):1551-1565
Mice
Wild-type mice and cardiomyocyte-specific GLP-1R knockout mice
Intraperitoneal injection
10 mg/kg
Single injection
To study the effects of GLP-1R agonists on heart rate in mice, results showed that both lixisenatide and liraglutide rapidly increased HR, and this effect was attenuated in cardiomyocyte-specific GLP-1R knockout mice.
Lixisenatide reduced infarct size by 36% in acute ischemia-reperfusion injury and improved left ventricular end-diastolic pressure and relaxation time, and prevented lung congestion in long-term treatment.
J Transl Med. 2013 Mar 28;11:84
C57BL/6N mice
Chronic unpredictable mild stress (CUMS) model
Intranasal administration
10 nmol/kg/d and 50 nmol/kg/d
Once daily from day 15 to day 40
Intranasal treatment of LXT significantly reduced immobility time, improved depressive and anxiety behaviors, and enhanced olfactory memory and sensitivity. Immunofluorescence analysis showed that LXT improved adult neurogenesis in the olfactory system and hippocampus.
Aging (Albany NY). 2021 Jan 10;13(3):3898-3908
Lixisenatide/利西拉来 技术信息
CAS号
320367-13-3
SMILES Code
NONE
MDL No.
MFCD13194768
别名
利西拉肽
;Lyxumia; Adlyxin; AVE0010; ZP10A peptide
运输
蓝冰
InChI Key
XVVOERDUTLJJHN-IAEQDCLQSA-N
Pubchem ID
90472060
存储条件
In solvent-20°C:3-6个月-80°C:12个月
Pure formSealed in dry, store in freezer, under -20°C
搜索
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