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  3. Lixisenatide

Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe−/− Irs2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Lixisenatide Chemical Structure

Lixisenatide Chemical Structure

CAS No. : 320367-13-3

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1 mg USD 150 In-stock
2 mg USD 220 In-stock
5 mg USD 290 In-stock
10 mg USD 390 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Lixisenatide

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe−/− Irs2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation[2][3][5].

IC50 & Target

MEK1

 

MEK2

 

MMP13

 

MMP-1

 

MMP-3

 

In Vitro

Lixisenatide (100 μM, 24 h) inhibits the Aβ25-35-induced cytotoxicity on cultured hippocampal cells. [1].
Lixisenatide (100 μM, 24 h) relieves the Aβ25-35-induced suppression of the Akt-MEK1/2 signaling pathway on cultured hippocampal cells [1].
Lixisenatide (10-20 μM, 48 h) ameliorates IL-1β-induced oxidative stress, mitochondrial dysfunction, and apoptosis in fibroblast-like synoviocytes (FLSs) [3].
Lixisenatide (10-20 μM, 48 h) reduces IL-1β-induced expression of MMPs and inhibits activation of proinflammatory pathways by IL-1β in FLSs[3].
Lixisenatide (10-20 μM, 6 h) reduced oxygen-glucose deprivation/reperfusion (OGD/R)-induced generation of ROS in HUVECs[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hippocampal cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Reversed Aβ25-35-triggered cytotoxicity on hippocampal cell cultures.

Western Blot Analysis[3]

Cell Line: FLSs
Concentration: 10 μM, 20 μM
Incubation Time: 48 h
Result: Significantly reduced expression of MMP-1, MMP-3, and MMP-13 at both the mRNA and protein levels in a dose-dependent manner.
In Vivo

Lixisenatide (10 μg/kg, Subcutaneous injection, once a day for a month) diminishes the atherosclerosis burden and produces more stable plaques [2].
Lixisenatide (10 μg/kg, Subcutaneous injection, once a day for a month) decreases systemic inflammation in atherogenic-diet-fed Apoe−/− Irs2+/− mice[2].
Lixisenatide (1 nmol/kg, Intraperitoneal injection, once a day for 14 days) afford renoprotective effects on experimental early diabetic nephropathy in a low dose[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Apoe−/− Irs2+/− mice [2]
Dosage: 10 μg/kg
Administration: Subcutaneous injection (s.c.)
Result: Exhibited smaller atheromas in the aortic arch region.
Reduced the lesion size in cross-sections of hearts.
Animal Model: Diabetic rats [4]
Dosage: 1 nmol/kg
Administration: Intraperitoneal injection (i.p.)
Result: Showed a significant amelioration on the elevated renal parameters.
Showed significant mitigation in renal MDA and total NOx (by 50.3 and 79.9%, respectively) and 43.9% elevation in renal total antioxidant capacity.
Averted the observed increments in iNOS and COX-2 expressions in the renal tissues of the diabetic group.
Decreased the level of TGF-β protein expression.
Clinical Trial
Molecular Weight

4858.49

Formula

C215H347N61O65S

CAS No.
Appearance

Solid

Color

White to pink

Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2

Sequence Shortening

HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (20.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2058 mL 1.0291 mL 2.0583 mL
5 mM 0.0412 mL 0.2058 mL 0.4117 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.2058 mL 1.0291 mL 2.0583 mL 5.1456 mL
5 mM 0.0412 mL 0.2058 mL 0.4117 mL 1.0291 mL
10 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5146 mL
15 mM 0.0137 mL 0.0686 mL 0.1372 mL 0.3430 mL
20 mM 0.0103 mL 0.0515 mL 0.1029 mL 0.2573 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Lixisenatide
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