Liraglutide (acetate) (Synonyms: NN 2211) |
| カタログ番号GC92125 |
Liraglutide (acetate)は膵高グルカゴン様ペプチド1（GLP-1）受容体の強力なアゴニストであり、パルミチン酸基を含むGLP-1（7-37）の合成誘導体でもある。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1997361-86-0
Sample solution is provided at 25 µL, 10mM.
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Liraglutide is a potent agonist of the glucagon-like peptide 1 (GLP-1) receptor and a synthetic derivative of GLP-1 (7-37) that contains a palmitic acid group.1 It increases cAMP accumulation in CHO cells expressing the human GLP-1 receptor (EC50 = 61 pM). Liraglutide (100-1,000 nM) inhibits cytokine- and free fatty acid-induced apoptosis of primary neonatal rat pancreatic β-cells in vitro by greater than 95 and 50%, respectively, effects that are blocked by the GLP-1 receptor antagonist exendin-3 (9-39) and the PI3 kinase inhibitor wortmannin.2 In a rat model of obesity induced by supplemental dietary candy, liraglutide (0.2 mg/kg, s.c., twice per day) decreases calorie intake, shifts food preference to a higher ratio of chow to candy, reverses weight and fat gains, and increases insulin sensitivity.3 Formulations containing liraglutide have been used as adjuncts in the treatment of type 2 diabetes and for chronic weight management in overweight or obese adults.
References:
[1]. Knudsen, L.B., Nielsen, P.F., Huusfeldt, P.O., et al.Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administrationJ. Med. Chem.43(9)1664-1669(2000).
[2]. Bregenholt, S., M?ldrup, A., Blume, N., et al.The long-acting glucagon-like peptide-1 analogue, liraglutide, inhibits beta-cell apoptosis in vitroBiochem. Bioph. Res. Commun.330(2)577-584(2005).
[3]. Raun, K., von Voss, P., Gotfredsen, C.F., et al.Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does notDiabetes56(1)8-15(2007).
| Cas No. | 1997361-86-0 | SDF | |
| 同義語 | NN 2211 | ||
| Chemical Name | L-histidyl-L-alanyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-α-glutamylglycyl-L-glutaminyl-L-alanyl-L-alanyl-N6-[N-(1-oxohexadecyl)-L-γ-glutamyl]-L-lysyl-L-α-glutamyl-L-phenylalanyl-L-isoleucyl-L-alanyl-L-tryptophyl-L-leucyl-L-valyl-L-arginylglycyl-L-arginyl-glycine, acetate | ||
| Canonical SMILES | O=C(CCCCCCCCCCCCCCC)N[C@@H](CCC(NCCCC[C@@H](C(N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@]([C@H](CC)C)([H])C(N[C@H](C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CCCNC(N)=N)C(NCC(O)=O)=O)=O)=O)=O)=O)=O)CC1=CNC2=C1C=CC=C2)=O)C)=O)=O)CC3=CC=CC=C3)=O)=O)NC([C@@H](NC([C@@H](NC([C@H](CCC(N)=O)NC(CNC([C@H](CCC(O)=O)NC([C@H](CC(C)C)NC([C@@H](NC([C@H](CO)NC([C@H](CO)NC([C@H](C(C)C)NC([C@@H](NC([C@H](CO)NC([C@@]([C@@H](C)O)([H])NC([C@@H](NC([C@@]([C@@H](C)O)([H])NC(CNC([C@H](CCC(O)=O)NC([C@@H](NC([C@@H](N[H])CC4=CN=CN4)=O)C)=O)=O)=O)=O)CC5=CC=CC=C5)=O)=O)=O)CC(O)=O)=O)=O)=O)=O)CC6=CC=C(O)C=C6)=O)=O)=O)=O)=O)C)=O)C)=O)=O)C(O)=O.CC(O)=O | ||
| Formula | C172H265N43O51? XC2H4O2 | M.Wt | 3811.3 |
| 溶解度 | DMSO: Slightly soluble,Water: Slightly soluble | Storage | -20°C |
| 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. |
||
| 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 | 0.2624 mL | 1.3119 mL | 2.6238 mL |
| 5 mM | 0.0525 mL | 0.2624 mL | 0.5248 mL |
| 10 mM | 0.0262 mL | 0.1312 mL | 0.2624 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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