UCT943|cas:1450666-80-4|西域试剂

UCT943,98.70%

产品编号：Bellancom-112435| CAS NO：1450666-80-4| 分子式：C₂₂H₂₀F₃N₅O| 分子量：427.42

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货号	价格	库存与货期
Bellancom-112435	￥5500.00	杭州北京（现货）
Bellancom-112435	￥9500.00	杭州北京（现货）
Bellancom-112435	￥29500.00	杭州北京（现货）

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UCT943

产品介绍

UCT943 是新一代恶性疟原虫 Plasmodium falciparum PI4K 抑制剂。UCT943 抑制 P. vivax PI4K (PvPI4K) 酶，IC₅₀ 为 23 nM。

生物活性

UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC₅₀ of 23 nM.

体外研究

UCT943 maintains high in vitro selectivity (>200-fold) for the parasite PvPI4K versus the human PI4Kβ isozyme (IC₅₀ of PI4Kβ, 5.4 μM), inhibition of which is linked to immunosuppressive effects.
In vitro cytotoxicity of UCT943 is tested against L6 cells, chinese hamster ovarian (CHO), Vero, and HepG2 cells, with 50% cytotoxic concentrations (CC₅₀s) of 12, 17, 113, and 13 μM, respectively.

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

体内研究

UCT943 shows excellent in vivo efficacy in the Plasmodium berghei (10 mg/kg and 3 mg/kg; oral administration; daily; 4 days) and P. falciparum NSG (NOD-scid IL-2Rγ^null) mouse models (0.01, 0.1, 0.3, 1.1 and 10 mg/kg; oral administration; once per day; 4 days). When dosed at 10 mg/kg per os (p.o.), UCT943 reduces parasitemia by >99.9% in the mouse P. berghei infection model and cures all mice, with >30 mean survival days (MSD). At 3 mg/kg p.o., no complete cure is achieved, and MSD is 10 days, albeit parasitemia is reduced by 99%. The resulting 90% effective dose (ED₉₀) is 1.0 mg/kg p.o. in the P. berghei infection model. The ED₉₀ is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.

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

Animal Model:	Mice with P. berghei and P. falciparum NOD-scid IL-2Rγ^null (NSG) models
Dosage:	10 mg/kg and 3 mg/kg for P. berghei model; 0.01, 0.1, 0.3, 1.1 and 10 mg/kg for P. falciparum NOD-scid IL-2Rγ^null (NSG) model
Administration:	Oral administration; daily; 4 days for P. berghei model Oral administration; once per day; 4 days for P. falciparum NOD-scid IL-2Rγ^null (NSG) model
Result:	The ED₉₀ is 1.0 mg/kg in the P. berghei infection model. The ED₉₀ is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.

体内研究

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

Animal Model:	Mice with P. berghei and P. falciparum NOD-scid IL-2Rγ^null (NSG) models
Dosage:	10 mg/kg and 3 mg/kg for P. berghei model; 0.01, 0.1, 0.3, 1.1 and 10 mg/kg for P. falciparum NOD-scid IL-2Rγ^null (NSG) model
Administration:	Oral administration; daily; 4 days for P. berghei model Oral administration; once per day; 4 days for P. falciparum NOD-scid IL-2Rγ^null (NSG) model
Result:	The ED₉₀ is 1.0 mg/kg in the P. berghei infection model. The ED₉₀ is 0.25 mg/kg in the P. falciparum-infected NSG mouse model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (584.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3396 mL	11.6981 mL	23.3962 mL
5 mM	0.4679 mL	2.3396 mL	4.6792 mL
10 mM	0.2340 mL	1.1698 mL	2.3396 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 (4.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.87 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 (4.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.87 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 (4.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.87 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。