FR122047 (hydrate)
目录号 : GC13132
selective inhibitor of COX-1
Sample solution is provided at 25 µL, 10mM.
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FR122047 is a selective inhibitor of cyclooxygenase (COX)-1 [1].
Cyclooxygenase (COX)-1 is constitutively expressed in almost all tissues. COX-1 gene has been considered to be a “housekeeping” gene. COX-1 has been responsible for the production of prostaglandins (PG) that are important for homeostatic functions, such as mediating normal platelet function, maintaining the integrity of the gastric mucosa, and regulating renal blood flow [2].
In recombinant human cyclooxygenase enzyme assays, FR122047 inhibited the activity of recombinant human cyclooxygenase-1 and cyclooxygenase-2 with the IC50 values of 0.028 ± 0.009 and 65 ± 19 μM for cyclooxygenase-1 and cyclooxygenase-2, respectively [1]. In MCF-7 cells, FR122047 treatment suppressed cell growth. Treatment with FR122047 apparently increased the ratio of Bax to Bcl-2, mitochondrial cytochrome c release, and apoptosis [3]. In rat type II collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA), oral administration of FR122047 showed anti-inflammatory effect in a dose-dependent manner with ED50 value of 0.56 mg/kg [4]. In guinea-pigs, oral administration of FR122047 inhibited arachidonic acid- and collagen-induced aggregation with an ED50 value of 280 μg/kg and 530 μg/kg, respectively [5].
References:
[1] Ochi T, Motoyama Y, Goto T. The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models[J]. European journal of pharmacology, 2000, 391(1): 49-54.
[2] Morita I. Distinct functions of COX-1 and COX-2[J]. Prostaglandins & other lipid mediators, 2002, 68: 165-175.
[3] Jeong H S, Kim J H, Choi H Y, et al. Induction of cell growth arrest and apoptotic cell death in human breast cancer MCF-7 cells by the COX-1 inhibitor FR122047[J]. Oncology reports, 2010, 24(2): 351.
[4] Ochi T, Goto T. Differential effect of FR122047, a selective cyclo‐oxygenase‐1 inhibitor, in rat chronic models of arthritis[J]. British journal of pharmacology, 2002, 135(3): 782-788.
[5] Dohi M, Sakata Y, Seki J, et al. The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor[J]. European journal of pharmacology, 1993, 243(2): 179-184.
| Cas No. | SDF | ||
| 化学名 | 1-[[4,5-bis(4-methoxyphenyl)-2-thiazolyl]carbonyl]-4-methyl-piperazine, monohydrochloride, monohydrate | ||
| Canonical SMILES | O=C(N1CCN(C)CC1)C2=NC(C3=CC=C(OC)C=C3)=C(S2)C4=CC=C(OC)C=C4.Cl | ||
| 分子式 | C23H25N3O3S • HCl [H2O] | 分子量 | 478.0 |
| 溶解度 | ≤1mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 2.0921 mL | 10.4603 mL | 20.9205 mL |
| 5 mM | 0.4184 mL | 2.0921 mL | 4.1841 mL |
| 10 mM | 0.2092 mL | 1.046 mL | 2.0921 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