中文名称: | RS504393 | ||||
---|---|---|---|---|---|
英文名称: | RS504393 | ||||
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-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one | ||||
CAS No: | 300816-15-3 | 分子式: | C25H27N3O3 | 分子量: | 417.5 |
CAS No: | 300816-15-3 | ||||
分子式: | C25H27N3O3 | ||||
分子量: | 417.5 | ||||
MDL: | MFCD09038564 |
基本信息
产品编号: |
R10038 |
||||
产品名称: |
RS504393 |
||||
CAS: |
300816-15-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
||||
分子式: |
溶于液体 |
-80℃ |
6个月 |
||
分子量: |
417.50 |
-20℃ |
1个月 |
||
化学名: |
6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one |
||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
|
|||
Ethanol |
|
||||
Water |
|
||||
体内(现配现用): |
|
||||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.3952mL |
11.9760mL |
23.9521mL |
5mM |
0.4790mL |
2.3952mL |
4.7904mL |
10mM |
0.2395mL |
1.1976mL |
2.3952mL |
生物活性
产品描述 |
一种选择性的CCR2拮抗剂,作用于人重组CCR2和CCR1受体,IC50分别为89nM和>100μM。 |
靶点 |
CCR |
体外研究 |
RS 504393 inhibits the MCP-1-induced chemotaxis with an IC50 of 330nM.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. |
体内研究 |
RS504393 (0.3-3μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice.RS 504393 (5mg/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. |
推荐实验方法(仅供参考)
激酶实验: |
Isolated mast cells are sensitized by incubation with anti-DNP IgE in RPMI1640 containing 10ng/mL of murine recombinant IL-3,10ng/mL of recombinant SCF,and 5% murine serum.The cells are then washed with HBSS containing 10ng/mL of murine recombinant IL-3,10ng/mL of recombinant SCF,0.04% BSA,and 10mM HEPES.Resuspended cells at a concentration of 2 to 8×104 cells/100μL are transferred into triplicate wells of a 96 well U-bottom plate and allowed to equilibrate at 37℃ for 10 minutes before the addition of DNP-albumin or compound 48/80.After 45 minutes,the plate is centrifuged at 290g for 5 minutes at 4℃.The β-hexosaminidase activity of the culture supernatant is determined using a Published protocol.Fifty-μL aliquots of the supernatant are placed in wells of another 96-well plate together with 100 L of 2.5mM p-nitrophenyl-N-acetyl β-d glucosaminide solubilized in 0.04mol/Lcitrate buffer adjusted to pH 4.5 with disodium phosphate.After incubation at 37℃ for 90 minutes,the reactions are terminated by addition of 50μL of 0.4mol/Lglycin adjusted to pH 10.7 with sodium hydroxide.The colored product is measured at 405nm with a reference filter of 570nm.The relative release of β-hexosaminidase is defined as the activity in the supernatant of the tested cells divided by the activity in the positive control cell supernatant,multiplied by 100.Compound 48/80 stimulus is used for assay control. |
动物实验: |
|
Male C57BL/6J mice (n=30) and male homozygote CCR1,CCR2 and CCR3 knockout mice (n=12,in each phenotype),6-8 weeks old and weighing 20±2g.Intranasal administration of PBS or LPS (5mg/kg) is performed in a volume of 1mL/kg body weight.C57BL/6J mice are treated with vehicle or RS504393 (5mg/kg) intraperitoneally 30 min before LPS challenge.Four hours after LPS challenge,mice are terminated by an intraperitoneal injection of an overdose of pentobarbitone.The mice are kept on a 12-h light/dark cycle with access to mice chow and water ad libitum. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )