PF-9184
目录号 : GC15351A potent mPGES-1 inhibitor
Cas No.:1221971-47-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PF-9184 is a novel mPGES-1 inhibitor [1]. Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal isomerase expressed in cytokine-sensitive brain endothelial cells. mPGES-1 functions as the central switch during immune-induced pyresis and as a target for treatment of fever and other PGE2-dependent acute phase reactions elicited by the brain [2]. mPGES-1 has been incolved in the formation of PGE2 essential for pain hypersensitivity and inflammation. Microsomal prostaglandin E synthase-1 (mPGES-1) has been involved in converting the COX product prostaglandin H2 (PGH2) into the biologically active PGE2[3].
In vitro: PF-9184 potently inhibited recombinant human mPGES-1 with an IC50 value of 16.5 ± 3.8 nM. PF-9184 showed no effect on rhCOX-1 and rhCOX-2 with >6500-fold selectivity. In rationally designed cell systems, PF-9184 inhibited PGE2 synthesis with IC50 in the range of 0.5–5 μM in serum-free cell and human whole blood cultures, while sparing the synthesis of 6-keto-PGF1α (PGF1α) and PGF2α[1]. PF-9184 showed no apparent cytotoxic effects up to 100 μM [1].
References:
[1] Mbalaviele G, Pauley A M, Shaffer A F, et al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor[J]. Biochemical pharmacology, 2010, 79(10): 1445-1454.
[2] Engblom D, Saha S, Engstrm L, et al. Microsomal prostaglandin E synthase-1 is the central switch during immune-induced pyresis[J]. Nature neuroscience, 2003, 6(11): 1137-1138.
[3] Jakobsson P J, Thorén S, Morgenstern R, et al. Identification of human prostaglandin E synthase: a microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target[J]. Proceedings of the National Academy of Sciences, 1999, 96(13): 7220-7225.
Cas No. | 1221971-47-6 | SDF | |
化学名 | N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide | ||
Canonical SMILES | OC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O | ||
分子式 | C21H14Cl2N2O4S | 分子量 | 461.3 |
溶解度 | ≤15mg/ml in DMSO;20mg/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 | 2.1678 mL | 10.8389 mL | 21.6779 mL |
5 mM | 0.4336 mL | 2.1678 mL | 4.3356 mL |
10 mM | 0.2168 mL | 1.0839 mL | 2.1678 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。