Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-actingglucagon-likepeptide-1 receptor agonist with anIC₅₀of 3.22 nM.

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

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 IC₅₀of 5 μM at 48 hour^[3].

Both low- and high-dose exendin-4 treatment inob/obmice improve serum ALT and reduce serum glucose, and calculated HOMA scores compared with control. Exendin-4-treatedob/obmice 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].

4186.57

Solid

C₁₈₄H₂₈₂N₅₀O₆₀S

141758-74-9

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

HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2

艾塞那肽

Room temperature in continental US; may vary elsewhere.

Protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

H₂O : 33.33 mg/mL(7.96 mM;Need ultrasonic)

DMSO : ≥ 32 mg/mL(7.64 mM)

Ethanol :< 1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

*"≥" means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 100 mg/mL (23.89 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
• 2.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

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

  此方案可获得 ≥ 2.5 mg/mL (0.60 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

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

  此方案可获得 ≥ 2.5 mg/mL (0.60 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 4.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

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

  此方案可获得 ≥ 2.5 mg/mL (0.60 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。