BMS-582949
目录号 : GC16997
A p38α MAP kinase inhibitor
Cas No.:623152-17-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: 13 nM
BMS-582949 is a p38 MAPK inhibitor
p38R MAP kinase plays a key role in regulating the biosynthesis of various inflammatory cytokines, such as tumor necrosis factor alpha and interleukin-1β. Thus, p38R inhibitors are considered as a promising therapy for inflammatory disease treatment.
In vitro: BMS-582949 was found to be 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective against Raf. Moreover, the binding mode of BMS-582949 with p38R was further demonstrated by X-ray crystallographic analyses [1].
In vivo: In a pseudoestablished rat adjuvant arthritis model, BMS-582949 at doses of 10 and 100 mg/kg was found to display dose-dependent reduction in paw swelling with qd dosing. In addition, with bid dosing at doses of 1 and 5 mg/kg, BMS-582949 showed improved efficacy, resulting in great reduction in paw swelling. Moreover, the statistically significant reduction in paw swelling was also observed with the treatment of BMS-582949 at doses as low as 0.3 mg/kg bid [1].
Clinical trial: A multicenter FDG-PET trial showed that in stable atherosclerosis, 12 weeks of treatment with BMS-582949 was not able to reduce arterial inflammation or hs-CRP when compared with placebo, while intensification of statin therapy could decrease arterial inflammation significantly [2].
References:
[1]. Liu C, et al. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl- N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases. J Med Chem. 2010 Sep 23;53(18):6629-39.
[2]. Emami H, et al. The effect of BMS-582949, a P38 mitogen-activated protein kinase (P38 MAPK) inhibitor on arterial inflammation: a multicenter FDG-PET trial. Atherosclerosis. 2015 Jun;240(2):490-6.
| Cas No. | 623152-17-0 | SDF | |
| 化学名 | 4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide | ||
| Canonical SMILES | O=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC | ||
| 分子式 | C22H26N6O2 | 分子量 | 406.48 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 15 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): slightly soluble | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL |
| 5 mM | 0.492 mL | 2.4601 mL | 4.9203 mL |
| 10 mM | 0.246 mL | 1.2301 mL | 2.4601 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet