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Taspoglutide

Cat. No. M21658
Taspoglutide Structure
Synonym:

ITM077; R1583; BIM51077

Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

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. Taspoglutide (R1583, BIM51077) 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.

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.

Chemical Information
Molecular Weight 3339.71
Formula C152H232N40O45
CAS Number 275371-94-3
Solubility (25°C) DMSO 40 mg/mL
Storage -20°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xin Zhang, et al. Cell Rep. Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes

[2] Zin Z Htike, et al. Diabetes Obes Metab. Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis

[3] Han-Qing Li, et al. Pharmazie. The efficacy of placebo-adjusted taspoglutide on body weight reduction in clinical trials

[4] S R K Seshasai, et al. Diabetes Obes Metab. Cardiovascular safety of the glucagon-like peptide-1 receptor agonist taspoglutide in people with type 2 diabetes: an individual participant data meta-analysis of randomized controlled trials

[5] Kjetil Retterstl. Expert Opin Investig Drugs. Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue

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Keywords: Taspoglutide, ITM077; R1583; BIM51077 supplier, GLP Receptor, inhibitors, activators


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