Pirinixic Acid Aminothiazole
目录号 : GC14323
A dual inhibitor of mPGES-1 and 5-LO
Cas No.:1492060-44-2
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
Pirinixic Acid Aminothiazole is a dual inhibitor of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase 1 (mPGES-1) with IC50 values of 0.3 and 0.4 μM, respectively [1].
5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1) are critical enzymes involved in the metabolism of arachidonic acid (AA). They are key enzymes in the synthesis of leukotrienes (LTs) and PGE2, respectively [1][2][3]. Dual inhibition of 5-LO and mPGES-1 is currently pursued as potential pharmacological strategy for treatment of inflammation and cancer [1].
Pirinixic Acid Aminothiazole is a dual inhibitor of 5-LO and mPGES-1. Pirinixic Acid Aminothiazole hardly inhibited cyclooxygenase (COX)-1/2 activities and failed to inhibit 12/15-LOs. In cell-free assay, Pirinixic Acid Aminothiazole was highly potent against both 5-LO and mPGES-1 with IC50 values of 0.3 and 0.4 μM, respectively. In the cell-based assay, Pirinixic Acid Aminothiazole inhibited 5-LO directly with IC50 value of 0.2 μM [1].
In zymosan-induced peritonitis in mice, Pirinixic Acid Aminothiazole (10 mg/kg) reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%, accompanied by significantly impaired levels of cysLTs (84% reduction) and PGE2 (46% reduction). These results suggested that Pirinixic Acid Aminothiazole dually inhibited LT and PGE2 synthesis in vivo connected to anti-inflammatory effectiveness [1].
References:
[1]. Hanke T, Dehm F, Liening S, et al. Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. J Med Chem. 2013 Nov 27;56(22):9031-44.
[2]. Funk CD. Prostaglandins and leukotrienes: advances in eicosanoid biology. Science. 2001 Nov 30;294(5548):1871-5.
[3]. Samuelsson B, Morgenstern R, Jakobsson PJ. Membrane prostaglandin E synthase-1: a novel therapeutic target. Pharmacol Rev. 2007 Sep;59(3):207-24.
| Cas No. | 1492060-44-2 | SDF | |
| 化学名 | 2-[[4-chloro-6-[[4-(2-naphthalenyl)-2-thiazolyl]amino]-2-pyrimidinyl]thio]-octanoic acid | ||
| Canonical SMILES | ClC1=NC(SC(CCCCCC)C(O)=O)=NC(NC2=NC(C3=CC=C(C=CC=C4)C4=C3)=CS2)=C1 | ||
| 分子式 | C25H25ClN4O2S | 分子量 | 513.1 |
| 溶解度 | ≤20mg/ml in DMSO;25mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9489 mL | 9.7447 mL | 19.4894 mL |
| 5 mM | 0.3898 mL | 1.9489 mL | 3.8979 mL |
| 10 mM | 0.1949 mL | 0.9745 mL | 1.9489 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。