Taspoglutide (ITM077) |
カタログ番号GC31360
One-Click Copy Product Info
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タスポグルチド (ITM077) は、2 型糖尿病の治療用に開発された長時間作用型グルカゴン様ペプチド 1 (GLP-1) 受容体アゴニストであり、EC50 値は 0.06 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 275371-94-3
Sample solution is provided at 25 µL, 10mM.
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Taspoglutide (ITM077) is a novel analog of human glucagon-like peptide-1 [hGLP-1(7-36)NH2] in clinical development for the treatment of type 2 diabetes. Taspoglutide inhibits VEGFR2 in CHO cells with an IC50 value of 4.6±0.6nM[1,2]. Taspoglutide is a structural derivative of hGLP-1 with α-aminoisobutyric acid (Aib) substitutions replacing Ala8 and Gly35[1].
In vitro, Taspoglutide (0.001-100nM) stimulates insulin secretion in a glucose-dependent manner, enhancing secretion at high glucose (16.7mM) even at very low concentrations (0.001nM) in INS-1E rat insulinoma cells[1].
In vivo, Taspoglutide (0.4mg; s.c.; once-monthly for 12 weeks) significantly decreased food intake and body weight in hyperglycemic ApoE-/- mice[3]. Taspoglutide (0.4mg; s.c.; once-monthly for 12 weeks) treatment significantly increased levels of mRNA transcripts for the transcription factor liver X receptor (Lxr) as well as multiple LXR target genes, Abca1, Abcg5, Abcg1, and Abcg8, involved in cholesterol shuttling and clearance. Taspoglutide (0.4mg; s.c.; once-monthly for 12wk) also increased mRNA levels for hepatic lipase (Hl), a key enzyme in the regulation of triglyceride storage and clearance, as well as Cpt1a, a ratelimiting mitochondrial fatty acid carrier regulating the rate of free fatty acid β-oxidation in hyperglycemic ApoE-/- mice[3]. Taspoglutide Treatment (1mg; s.c.; once) significantly reduced proliferating pancreatic β-cells per islet cross-section in ZDF rats[4].
References:
[1]. Sebokova, Elena, et al. "Taspoglutide, an analog of human glucagon-like peptide-1 with enhanced stability and in vivo potency." Endocrinology 151.6 (2010): 2474-2482.
[2]. Rosenstock, Julio, et al. "The fate of taspoglutide, a weekly GLP-1 receptor agonist, versus twice-daily exenatide for type 2 diabetes: the T-emerge 2 trial." Diabetes care 36.3 (2013): 498-504.
[3]. Panjwani, Naim, et al. "GLP-1 receptor activation indirectly reduces hepatic lipid accumulation but does not attenuate development of atherosclerosis in diabetic male ApoE−/− mice." Endocrinology 154.1 (2013): 127-139.
[4]. Uhles, S., et al. "Taspoglutide, a novel human once‐weekly GLP‐1 analogue, protects pancreatic β‐cells in vitro and preserves islet structure and function in the Zucker diabetic fatty rat in vivo." Diabetes, Obesity and Metabolism 13.4 (2011): 326-336.
| Cell experiment [1]: | |
Cell lines | MIN6B1 cells |
Preparation Method | MIN6B1 cells were cultured for 24h in MIN6 medium (DMEM-based) pH 7.0. The medium was then replaced by serum-free and low glucose (5mmol/l) MIN6 medium pH 7.0 containing 0, 0.1, 1, 10 or 100nM Taspoglutide. |
Reaction Conditions | 0, 0.1, 1, 10 or 100nM; 48h.0, 0.1, 1, 10 or 100nM; 48h. |
Applications | Taspoglutide stimulated the proliferation of dispersed islet cell. |
| Animal experiment [2]: | |
Animal models | Four-week-old male ApoE-/- mice |
Preparation Method | Four-week-old male ApoE-/- mice were started on a high-fat (45% kcal) diet. Modest hyperglycemia was induced using STZ (an initial dose of 75mg/kg followed by a second dose of 125mg/kg 10d later), and mice with glucose levels from 15-25mM were then randomized to different groups and treated for 12 weeks with a once-monthly s.c. 0.4mg Taspoglutide microtablet suspension, a s.c. placebo microtablet, or metformin (400mg/kg·d) continuously provided in the drinking water plus a s.c placebo microtablet. |
Dosage form | 0.4mg; s.c.; once-monthly for 12 weeks. |
Applications | Taspoglutide significantly decreased food intake and body weight. |
References: | |
| Cas No. | 275371-94-3 | SDF | |
| Canonical SMILES | [H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2] | ||
| Formula | C152H232N40O45 | M.Wt | 3339.71 |
| 溶解度 | DMSO : ≥ 28 mg/mL (8.38 mM) | Storage | Store at -20°C,Sealed storage, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 299.4 μL | 1.4971 mL | 2.9943 mL |
| 5 mM | 59.9 μL | 299.4 μL | 598.9 μL |
| 10 mM | 29.9 μL | 149.7 μL | 299.4 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)