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Taspoglutide

Name: Taspoglutide
Brand: TargetMol
SKU: T13091
Rating: 4.5 (1 reviews)

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Catalog No. T13091Cas No. 275371-94-3

Alias R1583, ITM077, BIM51077

Taspoglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (EC50 value of 0.06 nM) used for the treatment of type 2 diabetes.

Taspoglutide

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Catalog No. T13091Alias R1583, ITM077, BIM51077Cas No. 275371-94-3

Taspoglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (EC50 value of 0.06 nM) used for the treatment of type 2 diabetes.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
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100 mg	Inquiry	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	Taspoglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (EC50 value of 0.06 nM) used for the treatment of type 2 diabetes.
Targets&IC50	GLP1:（EC50）0.06 nM
In vitro	Taspoglutide (R1583/BIM51077), exhibiting 93% homology with native polypeptides, is a long-acting formulation of (Aib8-35) human GLP-1 (7-36 amides) that activates the GLP-1 receptor. It demonstrates an affinity constant (1.1±0.2 nM) towards the hGLP-1 receptor, closely mirroring the natural ligand’s affinity constant of 1.5±0.3 nM, and shows similar potency in stimulating cAMP production [2].
In vivo	The rate of glucose-induced insulin secretion from isolated enhanced by Taspoglutide, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide showed dose-dependent enhancement of glucose-dependent insulin release in Sprague-Dawley rats and diabetic db/db mice, thereby reducing blood glucose in the type 2 diabetic db/db mouse model[3]. Acute treatment with taspoglutide reduces glucose excursion and increased insulin response during oGTT. In chronically treated rats, glucose excursion and levels of GIP, PYY and triglycerides during oGTT on day 21 are significantly reduced[4]. Hepatic triglyceride levels are significantly reduced in livers from taspoglutide-treated. Taspoglutide does not reduce plaque area or lipid content in the aortic arch or abdominal aorta, and no significant change in aortic macrophage accumulation is detected after taspoglutide or metformin mice[5].
Synonyms	R1583, ITM077, BIM51077

Chemical Properties

Molecular Weight	3339.763
Formula	C₁₅₂H₂₃₂N₄₀O₄₅
Cas No.	275371-94-3
Smiles	CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O \|@@:205\|
Relative Density.	1.46
Sequence	His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-{Aib}-Arg-NH2
Sequence Short	{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 28 mg/mL (8.38 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (0.3 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.2994 mL	1.4971 mL	2.9942 mL	14.9711 mL
5 mM	0.0599 mL	0.2994 mL	0.5988 mL	2.9942 mL

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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