1. GPCR/G Protein
  2. Glucagon Receptor

Exendin-4 (Synonyms: Exenatide)

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

Exendin-4, 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
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5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Exendin-4:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Exendin-4, 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, insulin levels 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 insulin and 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
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 0.0239 mL 0.1194 mL 0.2389 mL
*Please refer to the solubility information to select the appropriate solvent.
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, insulin 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
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]

Storage
Protect from light
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.96%

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

Cat. No.: HY-13443