1. Immunology/Inflammation
  2. PGE synthase
  3. PF-4693627

PF-4693627 是一种有效的,口服生物可利用的,选择性的微粒体前列腺素E合酶 (mPGES-1) 抑制剂 (IC50=3 nM),可用于骨关节炎和类风湿关节炎等的研究。

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PF-4693627 Chemical Structure

PF-4693627 Chemical Structure

CAS No. : 1312815-93-2

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规格 价格 是否有货 数量
1 mg ¥2050
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5 mg ¥5125
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10 mg ¥8200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA)[1].

IC50 & Target

IC50: 3 nM (mPGES-1)[1]

体外研究
(In Vitro)

PF-4693627 also inhibits mPGES-1 with IC50s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively[1].
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model[1].
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t1/2=3.7 h) in Sprague-Dawley rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Guinea pig with carrageenan stimulated air pouch inflammation model[1]
Dosage: 10 mg/kg
Administration: Administered orally
Result: 63% PGE2 inhibition.
Animal Model: Sprague-Dawley rats[1].
Dosage: 1.0 mg/kg (Pharmacokinetic Analysis)
Administration: Administered i.v.
Result: Clearance (CL), volume of distribution (Vdss), t1/2, mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.
分子量

502.43

Formula

C26H29Cl2N3O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (199.03 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9903 mL 9.9516 mL 19.9033 mL
5 mM 0.3981 mL 1.9903 mL 3.9807 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.63%

参考文献

PF-4693627 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9903 mL 9.9516 mL 19.9033 mL 49.7582 mL
5 mM 0.3981 mL 1.9903 mL 3.9807 mL 9.9516 mL
10 mM 0.1990 mL 0.9952 mL 1.9903 mL 4.9758 mL
15 mM 0.1327 mL 0.6634 mL 1.3269 mL 3.3172 mL
20 mM 0.0995 mL 0.4976 mL 0.9952 mL 2.4879 mL
25 mM 0.0796 mL 0.3981 mL 0.7961 mL 1.9903 mL
30 mM 0.0663 mL 0.3317 mL 0.6634 mL 1.6586 mL
40 mM 0.0498 mL 0.2488 mL 0.4976 mL 1.2440 mL
50 mM 0.0398 mL 0.1990 mL 0.3981 mL 0.9952 mL
60 mM 0.0332 mL 0.1659 mL 0.3317 mL 0.8293 mL
80 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6220 mL
100 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4976 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
PF-4693627
目录号:
HY-125415
需求量: