2. MAPK/ERK Pathway
  3. p38 MAPK
  4. PF-03715455

PF-03715455 是一种有效的吸入的 p38 MAPK 抑制剂，对 p38α 有一定的选择性，对 p38α 和 p38β 的 IC50 值分别为 0.88 和 23 nM。PF-03715455 对 LPS 诱导的人全血 TNFα 产生有抑制作用 (IC50=1.7 nM)。PF-03715455 有用于慢性阻塞性肺病 (COPD) 的潜力。

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PF-03715455

PF-03715455 Chemical Structure

CAS No. : 1056164-52-3

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规格 价格 是否有货 数量
1 mg ￥400
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5 mg ￥1001
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10 mg ￥1602
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25 mg ￥3201
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50 mg ￥5441
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Customer Review

PF-03715455 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)[1][2].

IC50 & Target[1]

p38α

0.88 nM (IC50)

p38β

23 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
PBMC IC50
0.88 nM
Compound: 1ab, PF-03715455
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha preincubated for 40 mins prior to LPS-challenge by ELISA in the presence of 5 uM ATP
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha preincubated for 40 mins prior to LPS-challenge by ELISA in the presence of 5 uM ATP
[PMID: 21888439]
PBMC IC50
1.7 nM
Compound: 1ab, PF-03715455
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
[PMID: 21888439]
PBMC IC50
8 nM
Compound: PF-3715455
Inhibition of LPS-stimulated TNFalpha release in human PBMC cells preincubated for 1 hr followed by LPS stimulation and measured after 18 hrs
Inhibition of LPS-stimulated TNFalpha release in human PBMC cells preincubated for 1 hr followed by LPS stimulation and measured after 18 hrs
[PMID: 35546685]
体外研究
(In Vitro)

PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2].

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

PF-03715455 相关抗体:
体内研究
(In Vivo)

PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively[2].

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

Animal Model: Male CD Sprague Dawley rats (300-450 g)[2]
Dosage: 1 mg/kg
Administration: I.v. (Pharmacokinetic Analysis)
Result: The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively.
Clinical Trial
分子量

700.27

Formula

C35H34ClN7O3S2
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
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (71.40 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 1.4280 mL 7.1401 mL 14.2802 mL
5 mM 0.2856 mL 1.4280 mL 2.8560 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

只
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
参考文献

PF-03715455 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 1.4280 mL 7.1401 mL 14.2802 mL 35.7005 mL
5 mM 0.2856 mL 1.4280 mL 2.8560 mL 7.1401 mL
10 mM 0.1428 mL 0.7140 mL 1.4280 mL 3.5701 mL
15 mM 0.0952 mL 0.4760 mL 0.9520 mL 2.3800 mL
20 mM 0.0714 mL 0.3570 mL 0.7140 mL 1.7850 mL
25 mM 0.0571 mL 0.2856 mL 0.5712 mL 1.4280 mL
30 mM 0.0476 mL 0.2380 mL 0.4760 mL 1.1900 mL
40 mM 0.0357 mL 0.1785 mL 0.3570 mL 0.8925 mL
50 mM 0.0286 mL 0.1428 mL 0.2856 mL 0.7140 mL
60 mM 0.0238 mL 0.1190 mL 0.2380 mL 0.5950 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.

Keywords:

PF-037154551056164-52-3PF03715455PF 03715455p38 MAPKselectivityCOPDLPSTNFαproductioninhaledairwayinflammationInhibitorinhibitorinhibit

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目录号：
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