YS-121
目录号 : GC17979
Dual inhibitor of mPGES-1 and 5-LO
Cas No.:916482-17-2
Sample solution is provided at 25 µL, 10mM.
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YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) [1].
Cyclooxygenases (COX-1 and COX-2) have been involved in catalyzing the formation of prostaglandins and related eicosanoids and play an essential role in the pathogenesis of breast cancer. Actions of COX-2 are mediated by prostaglandin E2 (PGE2). Microsomal PGES-1 (mPGES-1), the inducible form of PGES, has a marked affinity for coupling with COX-2. Expression of mPGES-1 has been observed in inflammatory conditions and cancers of the stomach, colon, lung, endometrium, and skin [2].
YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM [1]. YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM [3]. YS-121 effectively inhibited PGE2 and LT synthesis in both cell free and intact cell assays. Intraperitoneal administration of YS-121 (1.5 mg/kg) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy [4]. YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively [1].
References:
[1] Koeberle A, Zettl H, Greiner C, et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase[J]. Journal of medicinal chemistry, 2008, 51(24): 8068-8076.
[2] Mehrotra S, Morimiya A, Agarwal B, et al. Microsomal prostaglandin E2 synthase‐1 in breast cancer: a potential target for therapy[J]. The Journal of pathology, 2006, 208(3): 356-363.
Werz O, Greiner C, Koeberle A, et al. Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid[J]. Journal of medicinal chemistry, 2008, 51(17): 5449-5453.
Koeberle A, Rossi A, Zettl H, et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2, 3-dimethylphenylamino) pyrimidin-2-ylthio) octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase[J]. Journal of Pharmacology and Experimental Therapeutics, 2010, 332(3): 840-848.
| Cas No. | 916482-17-2 | SDF | |
| 化学名 | 2-[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-octanoic acid | ||
| Canonical SMILES | CC1=C(NC2=CC(Cl)=NC(SC(C(O)=O)CCCCCC)=N2)C=CC=C1C | ||
| 分子式 | C20H26ClN3O2S | 分子量 | 408.0 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/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 | 2.451 mL | 12.2549 mL | 24.5098 mL |
| 5 mM | 0.4902 mL | 2.451 mL | 4.902 mL |
| 10 mM | 0.2451 mL | 1.2255 mL | 2.451 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