OC000459
(Synonyms: [5-氟-2-甲基-3-(喹啉-2-基甲基)吲哚-1-基]乙酸) 目录号 : GC12536
A potent, selective DP2 antagonist
Cas No.:851723-84-7,950688-14-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
OC000459 is a potent, selective and orally active antagonist of D prostanoid receptor 2 (DP2) with Ki value of 4nM [1].
DP2 is expressed on Th2 cells and eosinophils. It is activated by PGD2 which is reported to have effects on the pathogenesis of allergic disease. As an antagonist of DP2, OC000459 can prevent PGD2 from binding to human DP2 and rat recombinant DP2 with Ki values of 4nM and 3nM. In CHO cells expressing DP2, OC000459 suppresses PGD2 mediated calcium mobilization with IC50 value of 28nM. In human Th2 cells, OC000459 inhibits chemotaxis and production of IL-13 in response to PGD2 with IC50 values of 28nM and 19nM. In addition, oral administration of OC000459 effectively reduces blood eosinophilia in rats. OC000459 also shows inhibitory effect on the accumulation of eosinophil in guinea pigs aerosolized by DK-PGD2. Furthermore, OC000459 is also reported to inhibit the late-phase allergic response in patients with asthma [1, 2].
References:
[1] Pettipher R, Vinall S L, Xue L, et al. Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. Journal of Pharmacology and Experimental Therapeutics, 2012, 340(2): 473-482.
[2] Singh D, Cadden P, Hunter M, et al. Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. European Respiratory Journal, 2013, 41(1): 46-52.
| Cas No. | 851723-84-7,950688-14-9 | SDF | |
| 别名 | [5-氟-2-甲基-3-(喹啉-2-基甲基)吲哚-1-基]乙酸 | ||
| 化学名 | 2-[5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetic acid | ||
| Canonical SMILES | CC1=C(C2=C(N1CC(=O)O)C=CC(=C2)F)CC3=NC4=CC=CC=C4C=C3 | ||
| 分子式 | C21H17FN2O2 | 分子量 | 348.37 |
| 溶解度 | DMF: 0.5 mg/ml,DMSO: 1.1 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8705 mL | 14.3526 mL | 28.7051 mL |
| 5 mM | 0.5741 mL | 2.8705 mL | 5.741 mL |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8705 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。