TP-10|cas:898563-00-3|西域试剂

TP-10,99.33%

产品编号：Bellancom-14550| CAS NO：898563-00-3| 分子式：C₂₆H₁₉F₃N₄O| 分子量：460.45

TP-10是PDE10A 抑制剂, IC50 为0.8 nM。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14550	￥3500.00	杭州北京（现货）
Bellancom-14550	￥5000.00	杭州北京（现货）
Bellancom-14550	￥15000.00	杭州北京（现货）
Bellancom-14550	￥21000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

TP-10

产品介绍

TP-10 是一个选择性的 PDE10A 抑制剂，其 IC₅₀ 值为 0.8 nM。TP-10 具有抗氧化活性，对 DPPH 和 CUPRAC 的 IC₅₀ 值分别为 31.72 和 16.04 μg/ml。TP-10 可用于神经疾病的研究。

生物活性

TP-10 is a selective PDE10A inhibitor with an IC₅₀ value of 0.8 nM. TP-10 shows an antioxidant activity with IC₅₀s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy.

体外研究

TP-10 (10 μg /mL; 24 h) affects total reactive oxygen species in human brain-derived cells (U-87 MG).

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

Cell Viability Assay

Cell Line:	U-87 MG cells
Concentration:	10 μg/ml
Incubation Time:	24 hours
Result:	Decreased the total number of ROS-positive cells and showed no toxic effects to U-87 MG cells.

体内研究
(In Vivo)

TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides.

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

Animal Model:	Male CD rats
Dosage:	0.1, 0.32, 1.0, 3.2 and 10 mg/kg
Administration:	Subcutaneous injection; 0.1-10 mg/kg once
Result:	Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg.

体内研究

TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides.

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

Animal Model:	Male CD rats
Dosage:	0.1, 0.32, 1.0, 3.2 and 10 mg/kg
Administration:	Subcutaneous injection; 0.1-10 mg/kg once
Result:	Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg.

体内研究

TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides.

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

Animal Model:	Male CD rats
Dosage:	0.1, 0.32, 1.0, 3.2 and 10 mg/kg
Administration:	Subcutaneous injection; 0.1-10 mg/kg once
Result:	Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (217.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1718 mL	10.8589 mL	21.7179 mL
5 mM	0.4344 mL	2.1718 mL	4.3436 mL
10 mM	0.2172 mL	1.0859 mL	2.1718 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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.43 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.43 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 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.43 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。
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.38 mg/mL (5.17 mM); Clear solution

此方案可获得 ≥ 2.38 mg/mL (5.17 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 23.8 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

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213. [Content Brief]

. Schmidt CJ, et al. Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia. J Pharmacol Exp Ther. 2008 May;325(2):681-90. [Content Brief]

. Kaproń B, et al. 1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy. J Enzyme Inhib Med Chem. 2020 Dec;35(1):993-1002. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

TP-10,99.33%

TP-10

化学品安全说明书(MSDS)

质检证书(COA)

在线咨询