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Laflunimus
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。
Laflunimus图片
CAS NO:147076-36-6

HR325
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) -1-2抑制剂。
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 ofdihydroorotate dehydrogenase(DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50values of 2.5 and 2 μM forIgMandIgG, respectively. Laflunimus also is aprostaglandin endoperoxide H synthase (PGHS) -1and-2inhibitor[1][2].

体外研究
(In Vitro)

Ig secretion from mouse splenocytes was induced by lipopolysaccharide (LPS) for 5 days. Laflunimus inhibited the secretion of IgM and IgG with IC50values 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[1].
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)[2].

体内研究
(In Vivo)

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 ID50values of 38 mg/kg[1].

Animal Model:Male CD-1 mice (20-24 g)[1]
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.
分子量

310.27

性状

Solid

Formula

C15H13F3N2O2

CAS 号

147076-36-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.2230 mL16.1150 mL32.2300 mL
5 mM0.6446 mL3.2230 mL6.4460 mL
10 mM0.3223 mL1.6115 mL3.2230 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

*以上所有助溶剂都可在本网站选购。
 
 
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