Laflunimus - CAS:147076-36-6

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Laflunimus (Synonyms:HR325)

目录号 : KM4237 CAS No. : 147076-36-6 纯度 : 98%

Data Sheet 产品使用指南

Laflunimus (HR325) 是一种免疫抑制剂和 Leflunomide 活性代谢物 A771726 的类似物。Laflunimus 是一种口服的二氢硼酸脱氢酶 (DHODH) 抑制剂。Laflunimus 抑制免疫球蛋白 (Ig) 分泌，抑制 Ig M 和 IgG 分泌的 IC₅₀ 值分别为 2.5 和 2 μM。Laflunimus 也是前列腺素内过氧化物合酶 (PGHS) -1 和 -2 抑制剂。

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生物活性

Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC₅₀ values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.

体外研究

Ig secretion from mouse splenocytes was induced by lipopolysaccharide (LPS) for 5 days. Laflunimus inhibited the secretion of IgM and IgG with IC₅₀ values of 2.5 and 2 µM , respectively. Adding Uridine (50 µ M) increased these values to 70 and 60 µ M, respectively. Laflunimus inhibits LPS-induced kappa light-chain cell surface expression on 70Z/3 cells, a property also reversed by uridine.
Laflunimus (HR325) is more potent than A77 1726 as an inhibitor of PGHS in guinea pig polymorphonuclear leukocytes (IC₅₀= 415 and 4400 nM, respectively) and on isolated ovine PGHS-1 (IC₅₀=64 and 742 µM) and PGHS-2 (IC₅₀=100 and 2766 µM).

体内研究

HR325 (50 mg/kg; p.o.; days 14-18 after being injected with SRBC) inhibits the secondary anti-sheep red blood cell (SRBC) antibody response with ID₅₀ values of 38 mg/kg.

Animal Model:	Male CD-1 mice (20-24 g)
Dosage:	50 mg/kg
Administration:	Oral; days 14-18 after being injected with SRBC
Result:	The level of circulating anti-SRBC IgG in this model was inhibited dose relatedly by orally administered HR325.

分子式

C₁₅H₁₃N₂O₂F₃

分子量

310.27

CAS号

147076-36-6

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

溶解性数据

In Vitro:

DMSO : 50 mg/mL (161.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2230 mL	16.1150 mL	32.2300 mL
5 mM	0.6446 mL	3.2230 mL	6.4460 mL
10 mM	0.3223 mL	1.6115 mL	3.2230 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% corn oil
Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.06 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。