GW501516 (GSK-516, Cardarine)

製品コードS1473 バッチS147302

化学情報

	Synonyms	GW 1516 ,GSK-516	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₁₈F₃NO₃S₂
	分子量	453.50	CAS No.	317318-70-0
Solubility (25°C)*	体外	DMSO	91 mg/mL (200.66 mM)
		Ethanol	22 mg/mL (48.51 mM)
		Water	Insoluble
* <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	GW501516は、強力で高選択的なPPARβ/δアゴニストであり、hPPARαおよびhPPARγに対して1000倍の選択性を持ち、EC50は1 nMです。第4相。
in vitro	GW501516 is demonstrated to be 1000-fold more selective in comparison to existing subtypes. This compound increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts, and intestinal cells. It can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, this chemical is shown to block insulin resistance and fatty acid-induced nuclear factor-κB activation. It reduces the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity.
in vivo	GW501516 dramatically increases serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys. This compound induces fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles. Its treatment to mice fed a high-fat diet ameliorates diet-induced obesity as well as insulin resistance. This chemical also dramatically improves diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice.
特徴	A selective PPARδ agonist compared with a synthetic LXRα agonist GW3965.

プロトコル(参考用のみ)

キナーゼアッセイ	FA Binding Assays
キナーゼアッセイ	The PPARα, γ, and δ ligand-binding domains are expressed in E. coli as polyhistidine-tagged fusion proteins. The proteins are purified, biotinylated, and immobilized on streptavidin-modified SPA beads. [³H]this compound is used as radioligands for determination of binding to PPARα, γ, and δ, respectively. The buffer for all assays is 50 mM HEPES (pH 7), 50 mM KCl, 5 mM CHAPS, 0.1 mg/mg BSA, and 10 mM DTT.
動物実験	動物モデル	Male obese rhesus monkey
	投薬量	0.1, 0.3, 1.0, and 3.0 mg/kg
	投与方法	Orally

参考

https://pubmed.ncbi.nlm.nih.gov/12699745/
https://pubmed.ncbi.nlm.nih.gov/11309497/
https://pubmed.ncbi.nlm.nih.gov/10198642/

https://pubmed.ncbi.nlm.nih.gov/14525954/
https://pubmed.ncbi.nlm.nih.gov/20185762/
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2687435/
https://pubmed.ncbi.nlm.nih.gov/14676330/

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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：

Anlotinib Combined with Anti‐PD1 Potentiates Anti‐Tumor Immunity via Immunogenic Cell Death and Macrophage Reprogramming [ Adv Ther-Germany, 2023, 6, 2300141 ]	PubMed: None

Anlotinib Combined with Anti‐PD1 Potentiates Anti‐Tumor Immunity via Immunogenic Cell Death and Macrophage Reprogramming [ Adv Ther-Germany, 2023, 6, 2300141 ]

PubMed: None

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。

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