DSM502|cas:2426616-55-7|西域试剂

DSM502,99.57%

产品编号：Bellancom-132170| CAS NO：2426616-55-7| 分子式：C₁₆H₁₆F₃N₃O| 分子量：323.31

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	包装	价格	库存与货期	购买量	操作
Bellancom-132170		￥4000.00	杭州北京（现货）
Bellancom-132170		￥6400.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

DSM502

产品介绍

DSM502 是一种基于吡咯的二氢乳清酸脱氢酶 (DHODH) 抑制剂。DSM502 对 Plasmodium DHODH 和 Plasmodium 寄生虫表现出纳摩尔级效力，对哺乳动物 DHODH 没有抑制作用。

生物活性

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs.

体外研究

DSM502 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC₅₀=20 nM), P. vivax DHODH (PvDHODH, IC₅₀=14 nM) and Pf3D7 cells (EC₅₀=14 nM), with no inhibition of the human enzyme.

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

体内研究

DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study.
DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t_1/2 (2.6, 3.6 h) and C_max (8.4, 42.3 μM) in mice.
DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t_1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and V_ss (1.2 L/kg) in mice.

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

Animal Model:	SCID mice (23-36 g) were inoculated with parasites
Dosage:	10 and 50 mg/kg
Administration:	P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites
Result:	Resulted in 97% parasite clearance compared to 85% clearance in the GSK study. The 10 mg/kg mouse died on day 5.

体内研究

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

Animal Model:	SCID mice (23-36 g) were inoculated with parasites
Dosage:	10 and 50 mg/kg
Administration:	P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites
Result:	Resulted in 97% parasite clearance compared to 85% clearance in the GSK study. The 10 mg/kg mouse died on day 5.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (773.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0930 mL	15.4650 mL	30.9301 mL
5 mM	0.6186 mL	3.0930 mL	6.1860 mL
10 mM	0.3093 mL	1.5465 mL	3.0930 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: ≥ 2.08 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.43 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.43 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。