ONO-2952|cas:895169-20-7|西域试剂

ONO-2952,99.74%

产品编号：Bellancom-111191| CAS NO：895169-20-7| 分子式：C₂₂H₂₀ClFN₂O₂| 分子量：398.86

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-111191		￥9500.00	杭州北京（现货）
Bellancom-111191		￥16000.00	杭州北京（现货）

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ONO-2952

产品介绍

ONO-2952 是一种有效的，选择性的，口服活性的移位蛋白 18 kDa (TSPO) 拮抗剂，对大鼠和人 TSPO 的 K_i 值为 0.330-9.30 nM。与其他受体，转运蛋白，离子通道和酶相比，ONO-2952 对 TSPO 的选择性更高。ONO-2952 通过抑制大脑中的去甲肾上腺素能系统的过度激活而发挥其抗应激作用，并且不消除记忆。ONO-2952 可用于肠易激综合症。

生物活性

ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with K_i of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.

体外研究

As for its selectivity for TSPO, ONO-2952 at a concentration of 10 μM showed good selectivity for TSPO against 98 off-targets (<50% inhibition). Determination of ONO-2952 K_i or IC₅₀ values for the remaining 35 targets (50% inhibition at 10 μM) reveal K_i values of less than 1 μM only for 3 receptors, i.e. melatonin 2, progesterone B, and adrenergic α2C. The affinity of ONO-2952 for these receptors is at least 59 times lower than that for TSPO. ONO-2952 K_i value for the GABA_A receptor is more than 600 times higher than that for TSPO.

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

体内研究

ONO-2952 (0.03-3 mg/kg; oral administration; male Sprague Dawley rats) treatment dose-dependently suppresses restraint stress-induced defecation in rats with brain TSPO occupancy of more than 50%. ONO-2952 also suppresses conditioned fear stress-induced freezing behavior in rats.
ONO-2952 inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress.

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

Animal Model:	Male Sprague Dawley rats (8 weeks old) under conditioned fear stress test
Dosage:	0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:	Oral administration
Result:	Dose-dependently suppressed restraint stress-induced defecation in rats. And suppressed conditioned fear stress-induced freezing behavior in rats.

体内研究

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

Animal Model:	Male Sprague Dawley rats (8 weeks old) under conditioned fear stress test
Dosage:	0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:	Oral administration
Result:	Dose-dependently suppressed restraint stress-induced defecation in rats. And suppressed conditioned fear stress-induced freezing behavior in rats.

性状

Solid

溶解性数据

In Vitro:

DMSO : 180 mg/mL (451.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5071 mL	12.5357 mL	25.0715 mL
5 mM	0.5014 mL	2.5071 mL	5.0143 mL
10 mM	0.2507 mL	1.2536 mL	2.5071 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: 4.5 mg/mL (11.28 mM); Suspended solution; Need ultrasonic

此方案可获得 4.5 mg/mL (11.28 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 45.0 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% corn oil
Solubility: ≥ 4.5 mg/mL (11.28 mM); Clear solution

此方案可获得 ≥ 4.5 mg/mL (11.28 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 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。