|吡哆醇盐酸盐|CsnPharm

CAS No.: 586379-66-0

PH-797804/吡哆醇盐酸盐 Catalog No. CSN13463

Synonyms: N/A

PH-797804 is a pyridinone inhibitor of p38α with IC50 of 26 nM, being 4-fold selective versus p38β and does not inhibit JNK2.

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技术信息

生物活性

描述PH-797804 is a pyridinone inhibitor of p38α with IC50 of 26 nM, being 4-fold selective versus p38β and does not inhibit JNK2.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human monocytes	-	Function assay	-	Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced TNFalpha production, IC50=0.0034 μM	21620699
human PBMC	-	Function assay	-	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs, IC50=0.015 μM	21641211
human U937 cells	-	Function assay	-	Inhibition of p38alpha kinase-dependent HSP-27 phosphorylation in human U937 cells, IC50=0.00105 μM	21620699

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01314885	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> Pfizer Investigational Site London, United Kingdom, SE1 1YR Pfizer Investigational Site Manchester, United Kingdom, M23 9QZ Collapse <<
NCT00827515	Pain	Phase 1	Withdrawn	May 2009	-
NCT00383188	Arthritis, Rheumatoid	Phase 2	Completed	-	-

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参考文献

[1] Hope HR, Anderson GD, et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther. 2009 Dec;331(3):882-95.
[2] Xing L, Shieh HS, et al. Structural bioinformatics-based prediction of exceptional selectivity of p38 MAP kinase inhibitor PH-797804. Biochemistry. 2009 Jul 14;48(27):6402-11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0951 mL
- 10.4756 mL
- 20.9512 mL
- 5 mM
- 0.4190 mL
- 2.0951 mL
- 4.1902 mL
- 10 mM
- 0.2095 mL
- 1.0476 mL
- 2.0951 mL

技术信息

CAS号	586379-66-0	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C22H19BrF2N2O3	运输	蓝冰
分子量	477.30	别名	N/A

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01314885	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> Pfizer Investigational Site London, United Kingdom, SE1 1YR Pfizer Investigational Site Manchester, United Kingdom, M23 9QZ Collapse <<
NCT00827515	Pain	Phase 1	Withdrawn	May 2009	-
NCT00383188	Arthritis, Rheumatoid	Phase 2	Completed	-	-
NCT01226693	Healthy	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<
NCT01102660	Osteoarthritis	Phase 2	Completed	-	-
NCT01543919	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	-
NCT01479647	Healthy Volunteers	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<
NCT01217918	Healthy	Phase 1	Completed	-	United States, California ... more >> Pfizer Investigational Site Culver City, California, United States, 90232 Pfizer Investigational Site Glendale, California, United States, 91206 Collapse <<
NCT01924650	Healthy	Phase 1	Withdrawn	June 2014	-
NCT00620685	Arthritis, Rheumatoid	Phase 2	Completed	-	United States, Arizona ... more >> Pfizer Investigational Site Phoenix, Arizona, United States, 85013 United States, Colorado Pfizer Investigational Site Colorado Springs, Colorado, United States, 80909 United States, Florida Pfizer Investigational Site Miami, Florida, United States, 33169 United States, Maryland Pfizer Investigational Site Frederick, Maryland, United States, 21702 United States, Michigan Pfizer Investigational Site Bingham Farms, Michigan, United States, 48025 Pfizer Investigational Site Kalamazoo, Michigan, United States, 49007 United States, Pennsylvania Pfizer Investigational Site Duncansville, Pennsylvania, United States, 16635 Collapse <<
NCT02084485	Healthy	Phase 1	Completed	-	United Kingdom ... more >> Pfizer Investigational Site Denmark Hill, London, United Kingdom, SE5 9PJ Collapse <<
NCT00614705	Neuralgia, Postherpetic	Phase 2	Completed	-	Chile ... more >> Pfizer Investigational Site Vina del Mar, V Region, Chile, 2520997 Russian Federation Pfizer Investigational Site Moscow, Russian Federation, 123098 Pfizer Investigational Site St. Petersburg, Russian Federation, 194175 Pfizer Investigational Site St. Petersburg, Russian Federation, 194354 Pfizer Investigational Site Yaroslavl, Russian Federation, 150030 Spain Pfizer Investigational Site Cadiz, Spain, 11009 Pfizer Investigational Site Madrid, Spain, 28006 Pfizer Investigational Site Ourense, Spain, 32005 Pfizer Investigational Site Sevilla, Spain, 41013 Pfizer Investigational Site Valencia, Spain, 46014 Sweden Pfizer Investigational Site Linkoping, Sweden, 581 85 Pfizer Investigational Site Stockholm, Sweden, 114 54 Pfizer Investigational Site Stockholm, Sweden, 115 22 Ukraine Pfizer Investigational Site Dnipropetrovsk, Ukraine, 49616 Pfizer Investigational Site Donetsk, Ukraine, 83045 Pfizer Investigational Site Kharkiv, Ukraine, 61052 Pfizer Investigational Site Kharkiv, Ukraine, 61068 Pfizer Investigational Site Kharkiv, Ukraine, 61178 Pfizer Investigational Site Kyiv, Ukraine, 04050 Pfizer Investigational Site Odessa, Ukraine, 65025 Pfizer Investigational Site Simferopol, Ukraine, 95006 United Kingdom Pfizer Investigational Site Bexhill on Sea, East Sussex, United Kingdom, TN40 1JJ Pfizer Investigational Site Blackpool, Lancashire, United Kingdom, FY3 7EN Pfizer Investigational Site Weybridge, Surrey, United Kingdom, KT15 2BH Pfizer Investigational Site Solihull, United Kingdom, B91 2JL Collapse <<
NCT01862887	Healthy	Phase 1	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Collapse <<
NCT00559910	Chronic Obstructive Pulmonary ... more >>Disease Collapse <<	Phase 2	Completed	-	-
NCT01321463	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	-
NCT01589614	Healthy	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<

PH-797804/吡哆醇盐酸盐 Catalog No. CSN13463

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