URB937|cas:1357160-72-5|西域试剂

URB937,99.86%

产品编号：Bellancom-116477| CAS NO：1357160-72-5| 分子式：C₂₀H₂₂N₂O₄| 分子量：354.40

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货号	价格	库存与货期
Bellancom-116477	￥1600.00	杭州北京（现货）
Bellancom-116477	￥2800.00	杭州北京（现货）
Bellancom-116477	￥6000.00	杭州北京（现货）

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URB937

产品介绍

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)。

生物活性

URB937 is an orally active and peripherally restricted FAAH inhibitor (IC₅₀=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).

体外研究

URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus.
URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid.
URB937 in male rats (an oral dose 3 mg/kg, F = 36%) is absorbed at a moderate rate and displays a peak plasma concentration (C_max) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T_1/2 of 60 min by an oral dose of 3 mg/kg.
URB937 produces a high degree of antinociception in female mice and rats in models of visceral and inflammatory pain. Moreover, the compound displayed a restricted access to placental and fetal tissues in pregnant mice and rats.
URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Swiss Webster mice.
Dosage:	1 mg/kg.
Administration:	S.C.
Result:	Suppressesd pain responses elicited by i.p. injections of acetic acid.

Animal Model:	Adult Sprague Dawley male and female rats (250-300 g).
Dosage:	0.3, 1, 3, 10 mg/kg (Pharmacokinetic Analysis).
Administration:	Single oral dose.
Result:	Inhibited liver FAAH activity with a median effective dose (ED₅₀) of 0.9 mg/kg. Inhibits FAAH in peripheral tissues and identify a possible biomarker for target engagement.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Swiss Webster mice.
Dosage:	1 mg/kg.
Administration:	S.C.
Result:	Suppressesd pain responses elicited by i.p. injections of acetic acid.

Animal Model:	Adult Sprague Dawley male and female rats (250-300 g).
Dosage:	0.3, 1, 3, 10 mg/kg (Pharmacokinetic Analysis).
Administration:	Single oral dose.
Result:	Inhibited liver FAAH activity with a median effective dose (ED₅₀) of 0.9 mg/kg. Inhibits FAAH in peripheral tissues and identify a possible biomarker for target engagement.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (705.42 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8217 mL	14.1084 mL	28.2167 mL
5 mM	0.5643 mL	2.8217 mL	5.6433 mL
10 mM	0.2822 mL	1.4108 mL	2.8217 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。