RS 504393|300816-15-3|-陌孚医药/Medlife

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RS 504393

目录号: PC10644 纯度: ≥98%

CAS No. :300816-15-3

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中文名称

RS 504393

中文别名

6 - 甲基-1,1' - [2 - (5 - 甲基- 2-苯基- 4-恶唑基)乙基] - 螺[4H - 3-1,1 - 苯并恶嗪- 4,4' -哌啶]-2(1H)-酮;6-甲基-1,1''-[2-(5-甲基-2-苯基-4-恶唑基)乙基]-螺[4H-3-1,1-苯;6-甲基-1,1''-[2-(5-甲基-2-苯基-4-恶唑基)乙基]-螺[4H-3-1,1-苯并恶嗪-4,4''-哌啶]-2(1H)-酮;6-甲基-1,1-[2-(5-甲基-2-苯基-4-恶唑基)乙基]-螺[4H-3-1,1-苯并恶嗪-4,4-哌啶]-2(1H)-酮;6-甲基-1'-[2-(5-甲基-2-苯基-4-恶唑基)乙基]螺[4H-3,1-苯并恶嗪-4,4'-哌啶]-2(1H)-酮;6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one

英文名称

RS 504393

英文别名

6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one;6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro-[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one;6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one;RS 504393;6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one;ACMC-20a25e;CHEBI:317337;CHEMBL134074;CTK4G4374;MolPort-021-804-998;RS-504393;SureCN9972645;6-Methyl-1′-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4′-piperidin]-2(1H)-one;6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one;RS504393;GTPL781;HMS3269M19;HMS3677F05;HMS3413F05;BCPP000086;BCP02713

Cas No.

300816-15-3

分子式

C₂₅H₂₇N₃O₃

分子量

417.50

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

RS 504393 is a selective CCR2 chemokine receptor antagonist (IC₅₀ values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

性状

Solid

IC50 & Target[1][2]

CCR2

89 nM (IC₅₀)

Human α_1a receptor

72 nM (IC₅₀)

Human α_1d receptor

460 nM (IC₅₀)

5HT-1a receptor

1070 nM (IC₅₀)

体外研究(In Vitro)

RS 504393 inhibits the MCP-1-induced chemotaxis with an IC₅₀ of 330 nM. RS 504393 treatment suppresses allergen induced β-hexosaminidase release significantly. Without allergen priming, MCP-1 induces mast cell degranulation, which is completely suppressed by RS 504393.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181. [Information]

[2]. Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259. [Information]

[3]. Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246. [Information]

[4]. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. [Information]

[5]. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. [Information]

溶解度数据

体外研究:

DMSO : 12.5 mg/mL (29.94 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3952 mL	11.9760 mL	23.9521 mL
5 mM	0.4790 mL	2.3952 mL	4.7904 mL
10 mM	0.2395 mL	1.1976 mL	2.3952 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 50% DMSO 15% EtOH 35% PEG300
Solubility: 31.25 mg/mL (74.85 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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