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Redafamdastat {[allProObj[0].p_purity_real_show]}

货号:A137082 同义名: PF-04457845;PF-4457845 Ambeed 开学季,买赠积分,赢豪礼

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 CAS号:1020315-31-4
Redafamdastat 化学结构
CAS号:1020315-31-4
Redafamdastat 3D分子结构
CAS号:1020315-31-4
Redafamdastat 化学结构 CAS号:1020315-31-4
Redafamdastat 3D分子结构 CAS号:1020315-31-4
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Redafamdastat 纯度/质量文件 产品仅供科研

货号:A137082 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 FAAH 其他靶点 纯度
URB-597 ++++

FAAH, IC50: 4.6 nM

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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 {[allProObj[0].p_purity_real_show]}
PF-3845 ++

FAAH, Ki: 230 nM

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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]. PF-04457845 selectively inhibits FAAH with an IC50 of 7.2 nM[3]. Men aged 18–55 years with cannabis dependence were treated with PF-04457845 (4 mg per day), and they showed reduced symptoms of cannabis withdrawal, lower self-reported cannabis use and lower urinary THC-COOH concentrations, compared with placebo group[4]. Osteoarthritis patients administrated with 4 mg q.d. PF-04457845 showed decreased FAAH activity by >96% and significantly increased 4 endogenous substrates (fatty acid amides). PF-04457845 was well tolerated in osteoarthritis patients, and there was no evidence of cannabinoid-type adverse events, but failed to induce effective analgesia[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.

Redafamdastat 实验方案

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

CAS号1020315-31-4
分子式C23H20F3N5O2
分子量 455.432
别名 PF-04457845;PF-4457845;PF4457845, redafamdastat
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(230.55 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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