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BIA 10-2474

カタログ番号GC18174

BIA 10-2474 は、脂肪酸アミド加水分解酵素 (FAAH) の阻害剤であり、さまざまなラット脳領域での IC50 値は 50 ~ 70 mg/kg です。

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BIA 10-2474 化学構造

Cas No.: 1233855-46-3

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5mg
$54.00
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10mg
$95.00
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50mg
$284.00
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100mg
$450.00
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Sample solution is provided at 25 µL, 10mM.

Description of BIA 10-2474

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme). It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.

Protocol of BIA 10-2474

Animal experiment:

Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].

References:

[1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20.
[2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6

Chemical Properties of BIA 10-2474

Cas No. 1233855-46-3 SDF
Chemical Name N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
Canonical SMILES CN(C(N1C=NC(C2=C[N+]([O-])=CC=C2)=C1)=O)C3CCCCC3
Formula C16H20N4O2 M.Wt 300.4
溶解度 DMSO : 2.2 mg/mL (7.32 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of BIA 10-2474

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1 mg 5 mg 10 mg
1 mM 3.3289 mL 16.6445 mL 33.2889 mL
5 mM 0.6658 mL 3.3289 mL 6.6578 mL
10 mM 0.3329 mL 1.6644 mL 3.3289 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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