中文名称: RS504393
英文名称: RS504393
CAS No: 300816-15-3
分子式: C25H27N3O3
分子量: 417.5
R10038 RS504393 ≥98%(HPLC) (psaitong)
包装规格:
5mg 25mg in glass bottle
溶解性:
溶于DMSO(1mg/mL 加热)
产品描述:

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:

C25H27N3O3

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):