ML161 (Parmodulin 2)

製品コードS2916 バッチS291601

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	C₁₇H₁₇BrN₂O₂
	分子量	361.23	CAS No.	423735-93-7
Solubility (25°C)*	体外	DMSO	72 mg/mL (199.31 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	ML161 (Parmodulin 2) is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM.
in vitro	ML-161 is an allosteric inhibitor of PAR1. ML-161 displays dose-dependent inhibition of thrombin-induced platelet activation, as measured by P-selectin expression. ML-161 displays selective inhibition of SFLLRN and thrombin-induced platelet aggregation, both of which operate via PAR1, and has no effect on AYPGKF, thromboxane, or ADP-induced platelet aggregation, which are all agonists at alternative platelet GPCRs. ^[1]

製品説明

ML161 (Parmodulin 2) is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM.

in vitro

ML-161 is an allosteric inhibitor of PAR1. ML-161 displays dose-dependent inhibition of thrombin-induced platelet activation, as measured by P-selectin expression. ML-161 displays selective inhibition of SFLLRN and thrombin-induced platelet aggregation, both of which operate via PAR1, and has no effect on AYPGKF, thromboxane, or ADP-induced platelet aggregation, which are all agonists at alternative platelet GPCRs. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	P-Selectin Expression Assay
キナーゼアッセイ	Blood from healthy donors who has not ingested aspirin in the 2 weeks prior to donation is collected by venipuncture into 0.4% sodium citrate. Citrate-anticoagulated blood is centrifuged at 200g for 20 minutes to prepare platelet-rich plasma. Washed platelets are subsequently prepared from platelet-rich plasma by centrifugation at 1,000g in the presence of 0.15 μM PGE1. For analysis of P-selectin expression, 20 μL washed platelets (0.5-1 × 10⁸/mL) are incubated with the indicated agonists. Platelet activation is measured by P-selectin surface expression using PE-antihuman P-selectin and flow cytometry. Results are expressed as percent inhibition of P-selectin surface expression.

参考

[1] Dockendorff C, et al. ACS Med Chem Lett, 2012, 3(3), 232-237.

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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