SB 265610
目录号 : GC13458A selective CXCR2 inverse agonist
Cas No.:211096-49-0
Sample solution is provided at 25 µL, 10mM.
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SB 265610 is a potent CXCR2 antagonist that inhibits CINC-1-mediated Ca2+ mobilization with IC50 value of 3.4nM [1] [2].
CXCR2 is an integral membrane protein that specifically binds and responds to cytokines of the CXC chemokine family.
In isolated rat neutrophils stimulated with rat CINC-1, SB 265610 inhibited Ca2+ mobilization induced by CINC-1 with IC50 value of 3.4 nM in a dose-dependent way, while inhibited Ca2+ mobilization induced by C5a only with IC50 value of 6.8uM, which showed selectivity of the antagonist for CXCR2 [1]. In equilibrium saturation binding studies, SB265610 inhibited the binding of interleukin-8 without affecting the Kd. While, IL-8 couldn’t prevent binding of SB265610. SB265610 is an allosteric inverse agonist at the CXCR2 receptor [2].
In a hyperoxia rat model, newborn rats increased lung neutrophil content. Treatment with SB-265610 reduced hyperoxia-induced neutrophil accumulation in bronchoalveolar lavage and whole lung myeloperoxidase accumulation [1].
References:
[1]. Auten RL, Richardson RM, White JR, et al. Nonpeptide CXCR2 antagonist prevents neutrophil accumulation in hyperoxia-exposed newborn rats. J Pharmacol Exp Ther, 2001, 299(1): 90-95.
[2]. Bradley ME, Bond ME, Manini J, et al. SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor. Br J Pharmacol, 2009, 158(1): 328-338.
| Cas No. | 211096-49-0 | SDF | |
| 化学名 | 1-(2-bromophenyl)-3-(7-cyano-2H-benzo[d][1,2,3]triazol-4-yl)urea | ||
| Canonical SMILES | BrC1=CC=CC=C1NC(NC2=CC=C(C#N)C3=NNN=C23)=O | ||
| 分子式 | C14H9BrN6O | 分子量 | 357.16 |
| 溶解度 | 3mg/mL in DMSO, 3mg/mL in DMF, 5mg/mL in Ethanol | 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。 |
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| 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 | 2.7999 mL | 13.9993 mL | 27.9987 mL |
| 5 mM | 0.56 mL | 2.7999 mL | 5.5997 mL |
| 10 mM | 0.28 mL | 1.3999 mL | 2.7999 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