DSR-141562|cas:2007975-22-4|西域试剂

DSR-141562,99.98%

产品编号：Bellancom-136569| CAS NO：2007975-22-4| 分子式：C₁₉H₂₅F₃N₄O₃| 分子量：414.42

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货号	价格	库存与货期
Bellancom-136569	￥3800.00	杭州北京（现货）
Bellancom-136569	￥6500.00	杭州北京（现货）
Bellancom-136569	￥19500.00	杭州北京（现货）
Bellancom-136569	￥30000.00	杭州北京（现货）

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DSR-141562

产品介绍

DSR-141562 是一种新型的，具有口服活性的、可通透血脑屏障的磷酸二酯酶 (PDE) 抑制剂。DSR-141562 对人 PDE1B 具有优先选择性，IC₅₀ 为 43.9 nM，人 PDE1A 和 1C 的 IC₅₀ 值分别为 97.6 nM 和 431.8 nM。DSR-141562 用于精神分裂症相关症状及认知障碍的相关研究。

生物活性

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC₅₀ of 43.9 nM, and the IC₅₀ values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.

体外研究

体内研究

DSR-141562 (oral administration; 30 mg/kg; single dose; plasma and brain exposures 0.5, 1, 2, and 3 hours after administration) exhibits good brain uptake, with the brain-to-blood concentration ratio of unbound drug being 0.99 in rats.
DSR-141562 (oral administration; 10 mg/kg; single dose; 2 hours) slightly but significantly increases cGMP contents in the frontal cortex and striatum in rat.
DSR-141562 (oral administration; 30 mg/kg or 100 mg/kg; single dose; 2 hours) causes a significant increase in cGMP concentration in monkey CSF. The plasma concentrations of unbound this compound are above 43.9 nM (IC50s)for PDE1B in vitro (43.9 nM). DSR-141562 causes a significant increase in cGMP concentration in monkey CSF.
DSR-141562 (oral administration; 3 mg/kg, 10 mg/kg and 30 mg/kg; single dose) significantly reverses methamphetamine-induced locomotor hyperactivity, but has no effect on spontaneouslocomotor activity at 3 and 10 mg/kg.
DSR-141562 (oral administration; 0.3 mg/kg, 1 mg/kg or 3 mg/kg) significantly reversed the phencyclidine-induced decrease of social interaction time in mice.

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

Animal Model:	Male SpragueDawley rats
Dosage:	3 mg/kg, 10 mg/kg and 30 mg/kg
Administration:	Oral administration; single dose
Result:	Inhibited methamphetamine-induced locomotor hyperactivity in rats, while it had only minimal effects on the spontaneous locomotor activity.

Animal Model:	Male SpragueDawley rats
Dosage:	0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration:	Oral administration; single dose
Result:	Reversed social interaction.

体内研究

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

Animal Model:	Male SpragueDawley rats
Dosage:	3 mg/kg, 10 mg/kg and 30 mg/kg
Administration:	Oral administration; single dose
Result:	Inhibited methamphetamine-induced locomotor hyperactivity in rats, while it had only minimal effects on the spontaneous locomotor activity.

Animal Model:	Male SpragueDawley rats
Dosage:	0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration:	Oral administration; single dose
Result:	Reversed social interaction.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (60.33 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4130 mL	12.0651 mL	24.1301 mL
5 mM	0.4826 mL	2.4130 mL	4.8260 mL
10 mM	0.2413 mL	1.2065 mL	2.4130 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: ≥ 2.5 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.03 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。