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Avexitide

Name: Avexitide
Brand: TargetMol
SKU: TP2100
Price: 135 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: Exendin-3 (9-39) amide, Exendin (9-39)) Copy Product Info

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Synonyms: Exendin-3 (9-39) amide, Exendin (9-39)

Catalog No. TP2100 Copy Product Info

Purity: 99.65%

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Avexitide (Exendin-3(9-39)amide) is a specific, competitive GLP-1 receptor antagonist (Ki = 0.36 nM). Avexitide binds to the GLP-1 receptor (GLP-1R) with high affinity (Kd = 0.42 nM), blocking the interaction between endogenous GLP-1 and the receptor, thereby counteracting the effects of excessive GLP-1 secretion. Avexitide is being studied for post-bariatric hypoglycemia (PBH) and congenital hyperinsulinism.

Cas No. 133514-43-9

Pack Size	Price	USA Stock	Global Stock
500 µg	$135	In Stock	In Stock
1 mg	$198	In Stock	In Stock
5 mg	$529	In Stock	In Stock
10 mg	$753	In Stock	In Stock
25 mg	$1,130	-	In Stock
50 mg	$1,530	-	In Stock
100 mg	$1,980	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.65%

Appearance:Solid

Color:White

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COA HPLC MS

Product Introduction

Bioactivity

Description	Avexitide (Exendin-3(9-39)amide) is a specific, competitive GLP-1 receptor antagonist (Ki = 0.36 nM). Avexitide binds to the GLP-1 receptor (GLP-1R) with high affinity (Kd = 0.42 nM), blocking the interaction between endogenous GLP-1 and the receptor, thereby counteracting the effects of excessive GLP-1 secretion. Avexitide is being studied for post-bariatric hypoglycemia (PBH) and congenital hyperinsulinism.
Targets & IC50	GLP1:1.7 nM (Kd), GLP1 receptor:< 1.9 μM, GLP1 receptor:200 nM (EC50), exendin-3:20 nM
In vitro	Methods: Primary human pancreatic islet cells were co-cultured with Avexitide and the FATP2 inhibitor lipofermata (10 μM) under specific conditions to observe their effects on GLP-1 and insulin secretion. Results: The accompanying increase in insulin secretion was blocked by Avexitide. [1]
In vivo	Methods: An acute pain model was induced in mice by injecting capsaicin into the plantar surface of the hind paw. Thirty minutes prior to capsaicin injection, Avexitide was administered either locally into the plantar surface (0.1, 1, or 10 nmol/paw) or intraperitoneally (100 nmol/kg). Results: Avexitide Dose-dependent and significant attenuation of capsaicin-induced acute pain was observed. Local administration proved effective, suggesting a peripheral site of action. [2]
Synonyms	Exendin-3 (9-39) amide, Exendin (9-39)

Chemical Properties

Molecular Weight	3369.76
Formula	C₁₄₉H₂₃₄N₄₀O₄₇S
Cas No.	133514-43-9
Smiles	CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O
Relative Density.	1.51g/cm3
Sequence	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 Short	DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS

Storage & Solubility Information

Storage

Store at low temperature,Keep away from moisture,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 49 mg/mL (14.54 mM), Sonication is recommended.

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	0.2968 mL	1.4838 mL	2.9676 mL	14.8379 mL
5 mM	0.0594 mL	0.2968 mL	0.5935 mL	2.9676 mL
10 mM	0.0297 mL	0.1484 mL	0.2968 mL	1.4838 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc