1. GPCR/G Protein
  2. Glucagon Receptor
  3. Exendin-4

Exendin-4 (Synonyms: Exenatide)

Cat. No.: HY-13443 Purity: 98.96%
Handling Instructions

Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.

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

Exendin-4 Chemical Structure

Exendin-4 Chemical Structure

CAS No. : 141758-74-9

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1 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Exendin-4:

Top Publications Citing Use of Products

    Exendin-4 purchased from MCE. Usage Cited in: Front Pharmacol. 2019 Oct 25;10:1230.

    Exendin-4 or FSK treatment reduces ER stress-induced β-cell viability. INS-1 cells are incubated with THAP (0.5 μM), with Eexendin-4.

    Exendin-4 purchased from MCE. Usage Cited in: Front Pharmacol. 2019 Oct 25;10:1230.

    INS-1 cells are incubated with THAP (0.5 μM), H89, with Exendin-4 or FSK at indicated concentration for 24 h, then the IL-1β level is analyzed by qRT-PCR (n = 3).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.

    IC50 & Target

    IC50: 3.22 nM (glucagon-like peptide-1 receptor)[1]

    In Vitro

    In human umbilical vein endothelial cells, exendin-4 significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner[2]. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 μM at 48 hour[3].

    In Vivo

    Both low- and high-dose exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose, and calculated HOMA scores compared with control. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period[4]. Animals treated with exendin-4 have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats. Exendin-4 treatment is associated with lower leptin levels as well as lower HOMA values in rats[5]. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO[6].

    Clinical Trial
    Molecular Weight

    4186.57

    Formula

    C₁₈₄H₂₈₂N₅₀O₆₀S

    CAS No.

    141758-74-9

    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-Pro-Ser-NH2

    Sequence Shortening

    HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2

    SMILES

    [HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Protect from light
    Powder -80°C 2 years
      -20°C 1 year
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (7.64 mM)

    H2O : 1.23 mg/mL (0.29 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.2389 mL 1.1943 mL 2.3886 mL
    5 mM 0.0478 mL 0.2389 mL 0.4777 mL
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [4][5]

    Rats: 20 Sprague-Dawley male rats, ten of which are treated with exendin-4 (10 μg/kg) and ten of which are used as controls. The study period is 75 days. Serum and pancreatic tissue are removed for biochemical and histological study. Blood glucose, amylase, lipase and adipocytokines are compared between the two groups[5].

    Mice: The exendin-4 treatment groups are treated with 10 μg/kg every 24 hours for the first 14 days. This treatment is the induction phase. Respective control mice (lean and ob/ob) receive saline every 24 hours. After 14 days Exendin-4-treated mice are randomly divided into two groups: one group receives high dose exendin-4 (20 μg/kg) every 12 hours, while the second group continues with low dose exendin-4 (10 μg/kg) every 12 hours. The control mice continue to receive saline every 12 hours. The mice are weighed daily for the 60-day treatment period[4].

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

    References

    Purity: 98.96%

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    Product name:
    Exendin-4
    Cat. No.:
    HY-13443
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