受注:045-509-1970 |
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Synonyms | KDS-4103 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H22N2O3 |
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分子量 | 338.4 | CAS No. | 546141-08-6 | ||||
Solubility (25°C)* | 体外 | DMSO | 68 mg/mL (200.94 mM) | ||||
Ethanol | 4 mg/mL (11.82 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | URB597 (KDS-4103) is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1. |
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in vitro | URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH. [1] URB597 inhibits FAAH activity in human liver microsomes with IC50 of 3 nM. [2] URB597 reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide. [3] URB597 evokes Ca2+ entry in HEK293-F Cells transiently expressing human or rat TRPA1 gene. URB597 also activates Ca2+ entry in rat DRG neurons natively expressed TRPA1 channels. [4] |
in vivo | URB597 inhibits [3H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. URB597 enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH. [5] When delivered intraperitonealy (0.3 mg/kg) URB597 reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain. [6] URB597 reduces the reduction in body weight gain and sucrose intake induced by the chronic mild stress in rats through inhibition of brain FAAH activity. [7] URB597 could reverse most depressive-like symptoms induced by adolescent THC exposure in femal rats. [8] |
キナーゼアッセイ | Pharmacology | |
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Membrane fractions are prepared from brain homogenates, and FAAH activity is assayed using [3H]anandamide (anandamide[ethanolamine-3H], 60 Ci/mmol) as a substrate. Rat brain membranes (50 μg protein) are incubated for 30 min at 37 °C in buffer containing [3H]anandamide and varying concentrations of URB597. At the end of the incubation period, we stopp the reactions with a mixture of chloroform/methanol and measured [3H]ethanolamine in the aqueous phase by liquid scintillation counting. | ||
動物実験 | 動物モデル | Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice |
投薬量 | 0.3 mg/kg | |
投与方法 | Inject subcutaneously in a single dose 2 hours or 16 hours before killing |
Endocannabinoids regulate cocaine-associated memory through brain AEA-CB1R signalling activation [ Mol Metab, 2022, 65:101597] | PubMed: 36096452 |
Neuroprotective Effects of VEGF-A Nanofiber Membrane and FAAH Inhibitor URB597 Against Oxygen-Glucose Deprivation-Induced Ischemic Neuronal Injury [ Int J Nanomedicine, 2021, 16:3661-3678] | PubMed: 34093011 |
Fatty Acid Amide Hydrolase (FAAH) Inhibition Modulates Amyloid-Beta-Induced Microglia Polarization [ Int J Mol Sci, 2021, 22(14)7711] | PubMed: 34299330 |
Inhibition of fatty acid amide hydrolase prevents pathology in neurovisceral acid sphingomyelinase deficiency by rescuing defective endocannabinoid signaling [ EMBO Mol Med, 2020, e11776] | PubMed: 33016621 |
p21-activated kinase 1 restricts tonic endocannabinoid signaling in the hippocampus [ Elife, 2016, 5e14653] | PubMed: 27296803 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。