Liraglutide (acetate)
(Synonyms: NN 2211) 目录号 : GC92125Liraglutide (acetate)是胰高血糖素样肽1（GLP-1）受体的强效激动剂，也是含有棕榈酸基团的GLP-1（7-37）的合成衍生物。
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 | |
| 别名 | NN 2211 | ||
| 化学名 | 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 | ||
| 分子式 | C172H265N43O51? XC2H4O2 | 分子量 | 3811.3 |
| 溶解度 | DMSO: Slightly soluble,Water: Slightly soluble | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet