| Size | Price | Stock | Qty |
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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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Exenatide acetate (Exendin-4 Acetate), a bioactive peptide composed of 39 amino acids, is antidiabetic medication acting as a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. Exenatide, a synthetic version of endogenous glucagon-like peptide-1, suppresses hunger, inhibits the release of glucagon, increases insulin secretion, and slows stomach emptying. It is therefore utilized as supplemental therapy for diabetes mellitus.
| Targets |
glucagon-like peptide-1 receptor ( IC50 = 3.22 nM )
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|---|---|
| ln Vitro |
Exendin-4 dramatically and dose-dependently raises NO production, phosphorylation of endothelial NO synthase (eNOS), and GTP cyclohydrolase 1 (GTPCH1) in human umbilical vein endothelial cells[2]. MCF-7 breast cancer cells exhibit cytotoxic effects from exendin-4, with an IC50 of 5 μM after 48 hours[3].
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| ln Vivo |
Exendin-4 treatment, at both low and high doses, improves serum ALT and lowers serum glucose levels in ob/ob mice as well as computes HOMA scores in comparison to control. In the last four weeks of the study, the net weight gain of the ob/ob mice treated with extendin-4 is significantly reduced[4]. The Exendin-4-treated animals weigh a great deal less than the control rats and exhibit increased pyknotic nuclei and pancreatic acinar inflammation. Rats treated with extendin-4 have lower HOMA values and lower levels of leptin[5]. The rat thoracic aorta relaxes in response to exenatide in a dose-dependent manner. This relaxation is mediated primarily by H2S but also by NO and CO, and it is evoked through the GLP-1 receptor[6].
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| Animal Protocol |
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]. |
| References |
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| Molecular Formula |
C₁₈₆H₂₈₆N₅₀O₆₂S
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|---|---|
| Molecular Weight |
4246.62
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| CAS # |
914454-01-6
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| Related CAS # |
Exendin-4; 141758-74-9
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| Appearance |
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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| Synonyms |
Exendin-4 acetate; Exenatide acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
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. |
| Shipping Condition |
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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| Solubility (In Vitro) |
DMSO: ≥ 66.66 mg/mL (~15.7 mM)
H2O: ~25 mg/mL (~5.9 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (23.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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