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

Exendin-4 (Synonyms: Exenatide)

製品番号: HY-13443 純度: 98.96%
取扱説明書

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.

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Exendin-4 構造式

Exendin-4 構造式

CAS 番号 : 141758-74-9

容量 価格(税別) 在庫状況 数量
1 mg USD 72 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 168 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 252 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 360 在庫あり
Estimated Time of Arrival: December 31
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100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 11 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).
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    製品説明

    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]

    体外実験

    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].

    体内実験

    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].

    臨床実験
    分子量

    4186.57

    分子式

    C₁₈₄H₂₈₂N₅₀O₆₀S

    CAS 番号

    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]

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Protect from light
    Powder -80°C 2 years
      -20°C 1 year
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.
    体内:
    • 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.
    参考文献
    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 98.96%

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    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Exendin-4ExenatideExendin4Exendin 4Glucagon ReceptorGCGRInhibitorinhibitorinhibit

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    製品名:
    Exendin-4
    製品番号:
    HY-13443
    数量:
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