Liraglutide

製品コードS8256 バッチS825604

印刷

化学情報

Synonyms

NN2211, Liraglutida, Liraglutidum

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇₂H₂₆₅N₄₃O₅₁

分子量

3751.25

CAS No.

204656-20-2

Solubility (25°C)*

体外

Water

100 mg/mL (26.65 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

5.000mg/ml (1.33mM)

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Liraglutideは、長時間作用型グルカゴン様ペプチド-1(GLP-1)受容体作動薬です。
in vitro	Liraglutide attenuates induction of plasminogen activator inhibitor type-1 (PAI-1) and vascular adhesion molecule (VAM) expression in human vascular endothelial cells (hVECs) in vitro and may afford protection against endothelial cell dysfunction (ECD), an early abnormality in diabetic vascular disease. In vitro studies demonstrates GLP-1R-dependent this compound-mediated inhibition of stimulated PAI-1 and VAM expression.
in vivo	In vivo studies of vascular reactivity and immunohistochemical analysis are performed in the ApoE-/- mouse model. They demonstrate significant improvement in endothelial function in liraglutide treated mice, a GLP-1R dependent effect. This compound treatment also increases endothelial nitric oxide synthase (eNOS) and reduces intercellular adhesion molecule-1 (ICAM-1) expression in aortic endothelium, an effect again dependent on the GLP-1R. It reduces hyperglycemia in T2D mouse models by increasing pancreatic b cell mass through enhanced proliferation.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	human umbilical vein endothelial cell line C11-STH20
	濃度	100 nM
	反応時間	16 h
	実験の流れ	C11-STH cells are cultured to confluence at 37°C in gelatin-coated Nunclon cell culture dishes in Media-199 supplemented with penicillin/streptomycin, 20% FCS, 20 µg/ml endothelial cell growth factor and 20 µg/ml heparin. C11-STH cells are incubated under serum free conditions with liraglutide (100 nM) or the GLP-1 receptor antagonist exendin (9-39) (100 nM) alone or with 10 ng/ml TNFα for 16 h alone or in combination with this compound and/or exendin (9-39). ELISA assays for VCAM-1 and ICAM-1 are performed using conditioned medium from C11-STH cells to determine protein expression levels.
動物実験	動物モデル	Athymic nude mice
	投薬量	300 μg/kg/day
	投与方法	s.c.

参考

https://pubmed.ncbi.nlm.nih.gov/21517658/
https://pubmed.ncbi.nlm.nih.gov/26876561/
https://pubmed.ncbi.nlm.nih.gov/21562063/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Hypertonicity during a rapid rise in D-glucose mediates first-phase insulin secretion [ Frontiers in Endocrinology, June 25, 2024, 1395028]	PubMed: 38989001
A Brain Reward Circuit Inhibited By Next-Generation Weight Loss Drugs [ bioRxiv, December 17, 2024, nan]	PubMed: 39763823
Deleterious Effects of a GAD65 Monoclonal Autoantibody on Islet Function [ Diabetes, December 1, 2025, 2375-2389]	PubMed: 41071947
Liraglutide alleviates sepsis-induced encephalopathy via attenuating neuronal damage, glial cell activation and mitochondrial dysfunction in a mouse model of sepsis [ Research Square, August 27, 2025, nan]
Biased agonism of GLP-1R and GIPR enhances glucose lowering and weight loss, with dual GLP-1R/GIPR biased agonism yielding greater efficacy [ Cell Rep Med, 2025, 6(6):102156]	PubMed: 40460831
Enhancing Progestin Therapy with a Glucagon-Like Peptide 1 Agonist for the Conservative Management of Endometrial Cancer [ Cancers (Basel), 2025, 17(4)598]	PubMed: 40002193
An oncolytic vaccinia virus encoding hyaluronidase reshapes the extracellular matrix to enhance cancer chemotherapy and immunotherapy [ J Immunother Cancer, 2024, 12(3)e008431]	PubMed: 38458640
GLP-1R activation attenuates the progression of pulmonary fibrosis via disrupting NLRP3 inflammasome/PFKFB3-driven glycolysis interaction and histone lactylation [ J Transl Med, 2024, 22(1):954]	PubMed: 39434134
Hypertonicity during a rapid rise in D-glucose mediates first-phase insulin secretion [ Front Endocrinol (Lausanne), 2024, 15:1395028]	PubMed: 38989001
Targeting Clic1 for the treatment of obesity: A novel therapeutic strategy to reduce food intake and body weight [ Mol Metab, 2023, 76:101794]	PubMed: 37604246

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。