Vicriviroc Malate

製品コードS2004 バッチS200402

化学情報

	Synonyms	SCH 417690 (SCH-D) Malate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₈H₃₈F₃N₅O₂.C₄H₆O₅
	分子量	667.72	CAS No.	541503-81-5
Solubility (25°C)*	体外	DMSO	100 mg/mL (149.76 mM)
		Water	100 mg/mL (149.76 mM)
		Ethanol	100 mg/mL (149.76 mM)
* <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	Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.
in vitro	Vicriviroc binds with higher affinity to CCR5 versus SCH-C (SCH-351125) in competition binding assays with K_i value of 0.8 nM versus 2.6 nM. Vicriviroc is nearly 6-fold less active than SCH-C (IC50 = 5.8 μM versus 1.1 μM) in attenuating hERG current among voltage-clamped L929 cells, indicating a reduced potential for cardiac effects. Vicriviroc inhibits MIP-1α induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. In U-87-CCR5 cells, Vicriviroc inhibits intracellular calcium release induced by the ligand RANTES with IC50 of 16 nM, while Vicriviroc treatment alone does not stimulate the release of calcium. Vicriviroc inhibits GTPγS binding to the membranes from HTS-hCCR5 cells induced by RANTES, with IC50 of 4.2 nM. Vicriviroc displays potent antiviral activity against a panel of 30 R5-tropic HIV-1 isolates representing diverse genetic clades, with EC50 values ranging from 0.04 nM to 2.3 nM, and EC90 from 0.45 nM to 18 nM, being more potent (2- to 40-fold) than SCH-C. Vicriviroc is also highly active against a Clade G Russian isolate RU570 with EC90 of 16 nM, which is resistant to inhibition by SCH-C (EC90 > 1 μM). Vicriviroc could target an early step in the viral life cycle prior to reverse transcription and virion maturation, the targets of reverse transcriptase inhibitor and protease inhibitor, respectively. Consistent with the selectivity for CCR5, Vicriviroc is not active against viruses capable of using the CXCR4 coreceptor (R5/X4 or X4 tropic) for infection. ^[1]

製品説明

Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.

in vitro

Vicriviroc binds with higher affinity to CCR5 versus SCH-C (SCH-351125) in competition binding assays with K_i value of 0.8 nM versus 2.6 nM. Vicriviroc is nearly 6-fold less active than SCH-C (IC50 = 5.8 μM versus 1.1 μM) in attenuating hERG current among voltage-clamped L929 cells, indicating a reduced potential for cardiac effects. Vicriviroc inhibits MIP-1α induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. In U-87-CCR5 cells, Vicriviroc inhibits intracellular calcium release induced by the ligand RANTES with IC50 of 16 nM, while Vicriviroc treatment alone does not stimulate the release of calcium. Vicriviroc inhibits GTPγS binding to the membranes from HTS-hCCR5 cells induced by RANTES, with IC50 of 4.2 nM. Vicriviroc displays potent antiviral activity against a panel of 30 R5-tropic HIV-1 isolates representing diverse genetic clades, with EC50 values ranging from 0.04 nM to 2.3 nM, and EC90 from 0.45 nM to 18 nM, being more potent (2- to 40-fold) than SCH-C. Vicriviroc is also highly active against a Clade G Russian isolate RU570 with EC90 of 16 nM, which is resistant to inhibition by SCH-C (EC90 > 1 μM). Vicriviroc could target an early step in the viral life cycle prior to reverse transcription and virion maturation, the targets of reverse transcriptase inhibitor and protease inhibitor, respectively. Consistent with the selectivity for CCR5, Vicriviroc is not active against viruses capable of using the CXCR4 coreceptor (R5/X4 or X4 tropic) for infection. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Chemotaxis assay
キナーゼアッセイ	Ba/F3-CCR5 cells in chemotaxis buffer (RPMI supplemented with 1% FBS and 0.1 μg/mL mouse IL-3) are pretreated for 1 hour with increasing concentrations of Vicriviroc at 37 °C. Chemotaxis buffer containing Vicriviroc and MIP-1α (0.3 nM), MIP-1β (0.3 nM), or RANTES (0.3 nM) is placed into the bottom well of a 5-μm ChemoTx plate, and the filter unit is placed over the wells. Ba/F3-CCR5 cells pretreated with Vicriviroc are pipetted (25 μL) onto the filters, and the plate is incubated at 37 °C for 2 hours. Unmigrated cells are scraped off the filter, and the plate is centrifuged to pellet-migrated cells. Cells are then transferred to a Microlite 1⁺ Flatbottom Microtiter plate and quantitated using the Cell Titer Glow luminescent cell viability assay kit. IC50 value for Vicriviroc is calculated using GraphPad Prism Software.

参考

[1] Strizki JM, et al. Antimicrob Agents Chemother, 2005, 49(12), 4911-4919.

カスタマーフィードバック

: Data from [Nature, 2013, 493, 51-5]

: Data from [J Antimicrob Chemother, 2011, 66, 802-812]

: Data from [J Antimicrob Chemother, 2011, 66, 802-812]

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：

CCR5 is a receptor for Staphylococcus aureus leukotoxin ED. [Alonzo F 3rd, et al. Nature, 2013, 493(7430):51-5]	PubMed: 23235831
CCR5 antagonist blocks metastasis of basal breast cancer cells. [Velasco-Velázquez M, et al. Cancer Res, 2012, 72(15):3839-50]	PubMed: 22637726
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro. [Zembruski NC, et al. J Antimicrob Chemot, 2011, 66(4):802-12]	PubMed: 21393174
Decreased HIV diversity after allogeneic stem cell transplantation of an HIV-1 infected patient: a case report. [Kamp C, et al. Virol J, 2010, 7:55]	PubMed: 20210988

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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