Redafamdastat
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货号：A137082
同义名：
PF-04457845;PF-4457845
PF-04457845 selectively inhibits FAAH with an IC50 of 7.2 nM. It has anti-inflammatory effects and is used as analgesic.
Redafamdastat 化学结构
Redafamdastat 3D分子结构
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会员价
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+
Redafamdastat 质控信息
URB-597
++++
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JNJ-1661010
+++
FAAH (rat), IC50: 10 nM
FAAH (human), IC50: 12 nM
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Biochanin A
+
FAAH (mouse), IC50: 1.8 μM
FAAH (human), IC50: 1.4 μM
EGFR
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PF-3845
++
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Redafamdastat 生物活性
描述
Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide[3] 50 of 7.2 nM[3] [4] [5]
作用机制
PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH.
Redafamdastat 参考文献
[1] Johnson DS, Stiff C, et al. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96.
[2] Ahn K, Smith SE, et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24.
[3] Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96. doi: 10.1021/ml100190t. PMID: 21666860; PMCID: PMC3109749.
[4] D'Souza DC, Cortes-Briones J, Creatura G, Bluez G, Thurnauer H, Deaso E, Bielen K, Surti T, Radhakrishnan R, Gupta A, Gupta S, Cahill J, Sherif MA, Makriyannis A, Morgan PT, Ranganathan M, Skosnik PD. Efficacy and safety of a fatty acid amide hydrolase inhibitor (PF-04457845) in the treatment of cannabis withdrawal and dependence in men: a double-blind, placebo-controlled, parallel group, phase 2a single-site randomised controlled trial. Lancet Psychiatry. 2019 Jan;6(1):35-45. doi: 10.1016/S2215-0366(18)30427-9. Epub 2018 Dec 6. PMID: 30528676.
[5] Huggins JP, Smart TS, Langman S, Taylor L, Young T. An efficient randomised, placebo-controlled clinical trial with the irreversible fatty acid amide hydrolase-1 inhibitor PF-04457845, which modulates endocannabinoids but fails to induce effective analgesia in patients with pain due to osteoarthritis of the knee. Pain. 2012 Sep;153(9):1837-1846. doi: 10.1016/j.pain.2012.04.020. Epub 2012 Jun 21. PMID: 22727500.
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Redafamdastat 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.20mL
0.44mL
0.22mL
10.98mL
2.20mL
1.10mL
21.96mL
4.39mL
2.20mL
Redafamdastat 技术信息
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