Taspoglutide
Modify Date: 2024-01-02 23:06:04
Taspoglutide structure
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Common Name | Taspoglutide | ||
|---|---|---|---|---|
| CAS Number | 275371-94-3 | Molecular Weight | 3339.71000 | |
| Density | 1.46 | Boiling Point | N/A | |
| Molecular Formula | C152H232N40O45 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of TaspoglutideTaspoglutide 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. |
| Name | Taspoglutide |
|---|---|
| Synonym | More Synonyms |
| 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. |
|---|---|
| Related Catalog | |
| 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]. |
| 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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.46 |
|---|---|
| Molecular Formula | C152H232N40O45 |
| Molecular Weight | 3339.71000 |
| Exact Mass | 3337.71000 |
| PSA | 1385.09000 |
| LogP | 3.19740 |
| Storage condition | 2-8℃ |
| unii-2phk27ip3b |
| itm 077 |
| r 1583 |
| Taspoglutide Acetate |
- GL Biochem (Shanghai) Ltd.
- China
- Product Name: Taspoglutide Acetate
- Price: $Inquiry/1kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Jackie Yang
- DC Chemicals Limited
- China
- Product Name: Taspoglutide
- Price: $550.0/25mg
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Zhejiang Hangyu API Co., Ltd
- China
- Product Name: Taspoglutide
- Price: $Inquiry/1kg
- Purity: 99.0%
- Stocking Period: 1 Day
- Contact: Vinnie
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Price: $1763/10mM*1mLinDMSO
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