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FAAH

FAAH相关产品(12)
货号 产品名 中文名称 产品描述
SJ-MX2802 PF-3845 PF-3845 ia s highly selective and irreversible fatty acid amide hydrolase (FAAH) inhibitor.
SJ-MX3389 PF-04457845 PF-04457845 是一种高效选择性的 FAAH 抑制剂,作用于 hFAAH 和 rFAAH,IC50 分别为 7.2±0.63 nM 和 7.4±0.62 nM。
SJ-MX3498 JZL195 JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) (IC50 = 2 nM) and fatty acid amide hydrolase (FAAH) (IC50 = 4 nM), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. It poorly inhibits neuropathy target esterase and ABHD6 and does not inhibit other brain serine hydrolases. JZL 195 displays time-dependent inhibition of FAAH and MAGL in vivo, consistent with a covalent mechanism of activation.
SJ-MX3521 JNJ-42165279 JNJ-42165279 is a novel, potent, covalent and selective FAAH (fatty acid amide hydrolase) inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibited excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. The combination of good physical, ADME, and PD properties of JNJ-42165279 supported it entering the clinical portfolio.
SJ-MX2587 BIA 10-2474 BIA 10-2474 is a novel, potent, long-acting and reversible inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions. In a recent clinical trial, the drug BIA 10-2474 was responsible for severe adverse events (SAEs), including one death. To date, there has been little reliable information divulged about the potency of BIA 10-2474 at FAAH in the central nervous system.
SJ-MX1475 Carprofen 卡洛芬 Carprofen 是一种非甾体类抗炎剂,为多靶点 FAAH/COX 抑制剂,能够抑制 COX-2,COX-1 和 FAAH 的活性,IC50 值分别为 3.9 μM,22.3 μM 和 78.6 μM。
SJ-MX1394 JNJ-1661010 JNJ-1661010 (Takeda-25) 是一种有效的选择性脂肪酸酰胺水解酶 (FAAH) 抑制剂,对大鼠和人FAAH 的 IC50 分别为 34 和 33 nM。JNJ-1661010 可以穿透血脑屏障,可用于缓解疼痛的研究。
SJ-MX2679 FAAH-IN-2 FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a novel and potent FAAH (fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2. It is also named as O-Desmorpholinopropyl Gefitinib and is a metabolite of gefitinib, which is an EGFR inhibitor.
SJ-MX4105 PF 750 PF 750 is a novel, potent, selective and covalent/irreversible fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varying from 16.2-595 nM.
SJ-MX1111 URB937 URB937 是口服有效的、外周限制的 FAAH 抑制剂,IC50 值为 26.8 nM,可增加 anandamide 水平。URB937 不能影响脑内 FAAH 水平 (无法透过血脑屏障)。
SJ-MN0608 Biochanin A 鹰嘴豆芽素A,鸡豆黄素A Biochanin A 是一种天然存在的脂肪酸酰胺水解酶 (FAAH) 抑制剂,抑制FAAH,作用于小鼠,大鼠,人 FAAH,IC50 分别为 1.8,1.4 和 2.4 μM。
SJ-MX1959 URB-597 (KDS-4103) URB-597 (KDS-4103) 是一种有效的,具有口服活性的选择性 FAAH 抑制剂。 URB-597抑制大鼠脑膜中 FAAH 活性, IC50 为 5 nM,抑制体外大鼠神经元中FAAH 活性,IC50 为 0.5 nM,抑制人肝微粒体中FAAH 活性,IC50 为 3 nM。具有抗抑郁样作用和镇痛活性。