MRS 2578

製品コードS2855 バッチS2855

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₀N₆S₄
	分子量	472.67	CAS No.	711019-86-2
Solubility (25°C)*	体外	DMSO	42 mg/mL (88.85 mM)
		Water	Insoluble
		Ethanol	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	MRS 2578は、P2Y6受容体の強力なアンタゴニストであり、IC50は37 nMで、P2Y1、P2Y2、P2Y4、およびP2Y11受容体には有意な活性を示しません。
in vitro	MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. This compound (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. It inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. This chemical (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. It (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. The compound potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, it inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. This compound completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells.
in vivo	MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. This compound (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. This compound (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. This compound (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice.

プロトコル(参考用のみ)

動物実験	動物モデル	Murine endotoxinemia model
	投薬量	10 μM (100 μL)
	投与方法	Intravenous injection

参考

https://pubmed.ncbi.nlm.nih.gov/15081875/
https://pubmed.ncbi.nlm.nih.gov/21173118/
https://pubmed.ncbi.nlm.nih.gov/19422377/

https://pubmed.ncbi.nlm.nih.gov/21512170/

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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：

Baicalin inhibited PANX-1/P2Y6 signaling pathway activation in porcine aortic vascular endothelial cells infected by Glaesserella parasuis [ Heliyon, 2023 Dec 13, 10(1):e23632]	PubMed: 38187335
Blocking the A2B adenosine receptor alleviates myocardial damage by inhibiting spleen-derived MDSC mobilisation after acute myocardial infarction [ Ann Med, 2022, 54(1):1616-1626]	PubMed: 35675334
Adenosine deaminase modulates metabolic remodeling and orchestrates joint destruction in rheumatoid arthritis [ Sci Rep, 2021, 11(1):15129]	PubMed: 34301999

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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