1. GPCR/G Protein
  2. Glucagon Receptor
  3. Taspoglutide

Taspoglutide (Synonyms: ITM077; R1583; BIM51077)

Cat. No.: HY-P0165 Purity: 97.17%
Handling Instructions

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

For research use only. We do not sell to patients.

Taspoglutide Chemical Structure

Taspoglutide Chemical Structure

CAS No. : 275371-94-3

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1 mg USD 132 In-stock
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5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
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25 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

EC50: 0.06 nM (GLP-1)[1]

In Vitro

Taspoglutide (R1583/BIM51077) is a long acting 10% formulation of (Aib8-35) human GLP-1 (7-36 amides) with 93% homology with the native polypeptide. It activates the GLP-1 receptor. Taspoglutide has comparable affinity (affinity constant 1.1±0.2 nM) to the natural ligand (affinity constant 1.5±0.3 nM) for the hGLP-1 receptor and exhibits comparable potency in stimulating cAMP production[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Taspoglutide has been shown to enhance the rate of glucose-induced insulin secretion from isolated, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide in Sprague-Dawley rats and diabetic db/db mice have shown a dose-related enhancement of glucose-dependent insulin release, which lower blood glucose in the db/db mouse model of type 2 diabetes[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

3339.71

Formula

C₁₅₂H₂₃₂N₄₀O₄₅

CAS No.

275371-94-3

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 Shortening

H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2

SMILES

[H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (8.38 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2994 mL 1.4971 mL 2.9943 mL
5 mM 0.0599 mL 0.2994 mL 0.5989 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[4][5]

Rats: The Zucker diabetic fatty (ZDF) rats (animal model of type 2 diabetes) are used in the study. ZDF rats are treated acutely (0.1, 1, 10 μg/kg) or chronically (sustained-release of 1 mg) with a single long-acting dose of taspoglutide. Pioglitazone is used as a positive control in the chronic study. Postprandial glucose, body weight, glycaemic control and insulin sensitivity are assessed over 21 days in chronically treated animals[4].

Mice: High-fat diet-fed male ApoE-/- mice are used in the study. Mice with glucose levels from 15-25 mM are then randomized to different groups and treated for 12 wk with a once-monthly sc 0.4-mg taspoglutide microtablet suspension, a sc placebo microtablet, or metformin (400 mg/kg*d) continuously provided in the drinking water plus a sc placebo microtablet[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

TaspoglutideITM077 R1583 BIM51077ITM 077ITM-077R1583R 1583R-1583BIM51077BIM 51077BIM-51077Glucagon ReceptorGCGRInhibitorinhibitorinhibit

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Taspoglutide
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