WR99210

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WR99210

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

47326-86-3

WR99210 是一种口服有效的、低毒的二氢叶酸还原酶 (DHFR) 抑制剂 (IC₅₀<0.075 nM)。WR99210 具有较好的抗寄生虫活性，能有效抑制间日疟原虫和恶性疟原虫株 (包括耐 Pyrimethamine (HY-18062) 的恶性疟原虫株) 以及弓形虫。

生物活性

WR99210 is an orally active and low-toxicitydihydrofolate reductase (DHFR)inhibitor (IC₅₀<0.075 nM). WR99210 shows good antiparasitic activity and is effective againstP. falciparumandP. falciparumstrains (includingPyrimethamine(HY-18062)-resistantP. falciparumstrains) as well asT. gondii^[1]^[2]^[3].

IC₅₀& Target

IC50:<0.075 nM (DHFR)^[3].

体外研究
(In Vitro)

WR99210 (0-100 nM; 92 h) is highly effective againstT. gondiitachyzoites in tissue culture^[1].
WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts^[1].

Cell Viability Assay^[1]

Cell Line:	Human foreskin fibroblasts (T. gondii-infected)
Concentration:	0-100 nM
Incubation Time:	92 h
Result:	Showed marked inhibition ofT. gondii, with an IC₅₀value of approximately 50 nM.

Cell Cytotoxicity Assay^[1]

Cell Line:	Human foreskin fibroblasts
Concentration:	0-100 nM
Incubation Time:	92 h
Result:	Lacked of toxicity for fibroblasts.

体内研究
(In Vivo)

WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective againstT. gondiitachyzoites in a mouse model^[1].

Animal Model:	Male mice (T. gondii-infected)^[1].
Dosage:	1.25 mg/kg
Administration:	Intraperitoneal injection; single daily for 5 days.
Result:	Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5.

分子量

394.68

性状

Solid

Formula

C₁₄H₁₈Cl₃N₅O₂

CAS 号

47326-86-3

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

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

DMSO : 5 mg/mL(12.67 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.5337 mL	12.6685 mL	25.3370 mL
5 mM	0.5067 mL	2.5337 mL	5.0674 mL
10 mM	0.2534 mL	1.2668 mL	2.5337 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。