规格 | 价格 | 库存 | 数量 |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
glucagon-like peptide-1 receptor ( IC50 = 3.22 nM )
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体外研究 (In Vitro) |
在人脐静脉内皮细胞中,Exendin-4 以剂量依赖性方式显着增加 NO 产生、内皮 NO 合酶 (eNOS) 磷酸化和 GTP 环水解酶 1 (GTPCH1) 水平 [2]。 Exendin-4 对 MCF-7 乳腺癌细胞显示出细胞毒性作用,48 小时时 IC50 为 5 μM[3]。
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体内研究 (In Vivo) |
与对照组相比,低剂量和高剂量 Exendin-4 治疗 ob/ob 小鼠均可改善血清 ALT 并降低血糖,并计算出 HOMA 评分。 Exendin-4 治疗的 ob/ob 小鼠在研究期的最后 4 周内净体重增加显着减少[4]。与对照大鼠相比,用 Exendin-4 治疗的动物有更多的胰腺腺泡炎症、更多的核固缩且体重显着减轻。 Exendin-4 治疗与大鼠体内瘦素水平降低以及 HOMA 值降低相关[5]。艾塞那肽引起大鼠胸主动脉的剂量依赖性松弛,这是通过 GLP-1 受体引起的,主要由 H2S 介导,也由 NO 和 CO 介导[6]。
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动物实验 |
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. There are 75 days in the study period. Pancreatic tissue and serum are extracted for histological and biochemical analysis. The two groups' levels of blood glucose, lipase, amylase, and adipocytokines are compared[5].
Mice: For the first 14 days, 10 μg/kg is administered to the exendin-4 treatment groups every 24 hours. This therapy is the initiating stage. Every 24 hours, the corresponding control mice (lean and ob/ob) are given saline. Exendin-4-treated mice are split into two groups at random after 14 days: the first group is given a high dose of exendin-4 (20 μg/kg) every 12 hours, while the second group is given a low dose of exendin-4 (10 μg/kg) every 12 hours. Every twelve hours, saline is still given to the control mice. Every day for the duration of the 60-day treatment, the mice are weighed[4]. |
参考文献 |
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分子式 |
C₁₈₆H₂₈₆N₅₀O₆₂S
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分子量 |
4246.62
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CAS号 |
914454-01-6
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相关CAS号 |
Exendin-4; 141758-74-9
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外观&性状 |
Powder
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SMILES |
CC[C@H](C)[C@@H](CN[C@@H](CCC(=O)O)CN[CH]CN[C@@H](CC(C)C)CN[C@@H](CCCCN)CN[C@@H](CC(=O)N)CNCCNCCN1CCC[C@H]1CN[C@H](CN[C@H](CNCCN[CH]CN2CCC[C@H]2CN3CCC[C@H]3CN4CCC[C@H]4CN[C@H](CN)CO)CO)CO)NC[CH]NC[C@H](CC(C)C)NC[CH]
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InChi Key |
PIJVPWRREHDVDN-IFKXHDEJSA-N
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InChi Code |
InChI=1S/C76H159N22O6/c1-8-61(7)74(88-31-29-85-45-64(86-9-2)40-59(3)4)53-94-63(21-22-76(103)104)44-84-28-30-87-65(41-60(5)6)49-89-62(16-10-11-23-77)48-90-66(42-75(79)102)46-82-26-24-80-32-38-95-34-12-17-70(95)51-93-69(58-101)50-91-68(57-100)47-83-27-25-81-33-39-96-35-14-19-72(96)54-98-37-15-20-73(98)55-97-36-13-18-71(97)52-92-67(43-78)56-99/h2,28-29,33,59-74,80-94,99-101H,8-27,30-32,34-58,77-78H2,1,3-7H3,(H2,79,102)(H,103,104)/t61-,62-,63-,64-,65-,66-,67+,68+,69+,70-,71-,72-,73-,74+/m0/s1
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别名 |
Exendin-4 acetate; Exenatide acetate
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: ≥ 66.66 mg/mL (~15.7 mM)
H2O: ~25 mg/mL (~5.9 mM) |
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溶解度 (体内) |
配方 1 中的溶解度: 100 mg/mL (23.55 mM) in PBS (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液; 超声助溶。
请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 0.2355 mL | 1.1774 mL | 2.3548 mL | |
5 mM | 0.0471 mL | 0.2355 mL | 0.4710 mL | |
10 mM | 0.0235 mL | 0.1177 mL | 0.2355 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Exendin-4 (Ex-4; a form of exenatide) increases nitric oxide (NO) production, endothial nitric oxide synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in human umbilical vein endothelial cells (HUVECs). Am J Physiol Endocrinol Metab . 2016 Jun 1;310(11):E947-57. td> |
The effect of Exendin-4 administration on the rate of net weight gain in ob/ob and their lean littermates. Hepatology . 2006 Jan;43(1):173-81. td> |
Assessment of lipid content and hepatic histology in the liver of ob/ob mice and their lean littermates after Exendin-4 treatment. Hepatology . 2006 Jan;43(1):173-81. td> |
TBAR measurements following Exendin-4 treatment reveals that high-dose therapy resulted in significant reduction in oxidative stress. Hepatology . 2006 Jan;43(1):173-81. td> |
Effect of exenatide on the vasoactivity of rat thoracic aorta. Cardiovasc Diabetol . 2014 Apr 2:13:69. td> |
Role of GLP-1 receptor and endothelial denudation in the vasodilatation due to exenatide. Cardiovasc Diabetol . 2014 Apr 2:13:69. td> |