Iguratimod

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Iguratimod

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:

123663-49-0

艾拉莫德
T614

Iguratimod 是一种抗风湿剂，能够有效地抑制COX-2的活性，IC₅₀值为 20 μM (7.7 μg/mL)，而对 COX-1 无作用；Iguratimod 同时为巨噬细胞移动抑制因子 (MIF) 抑制剂，IC₅₀值为 6.81 μM。

生物活性

Iguratimod is an antirheumatic agent, acts as an inhibitor ofCOX-2, with anIC₅₀of 20 μM (7.7 μg/mL), but shows no effect onCOX-1. Iguratimod also inhibitsmacrophage migration inhibitory factor(MIF) with anIC₅₀of 6.81 μM.

IC₅₀& Target^[1]^[3]

COX-2

20 μM (IC₅₀)

MIF

6.81 μM (IC₅₀)

体外研究
(In Vitro)

Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC₅₀of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod (0.1, 1, 10 μg/mL) inhibits bradykinin-stimulated PGE2 release from fibroblasts. Iguratimod suppresses the COX activity from bradykinin stimulated fibroblasts in a concentration-dependent manner, with an IC₅₀of 48 μg/mL. Iguratimod (10 and 30 μg/mL) also dose-dependently inhibits COX-2 mRNA levels^[1]. In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC₅₀of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro^[3].

体内研究
(In Vivo)

Iguratimod (5 or 20 mg/kg) shows analgesic effect, significantly improves the pain withdrawal threshold of the left hind paw in dose-dependent manner in rats. Iguratimod (5 or 20 mg/kg) reduces the elevation of pERK1/2 and c-Fos in the spinal cord induced by cancer cell inoculation. Iguratimod also dose-dependently decreases the IL-6 levels in rats. In Iguratimod-treated rats, the activity of osteoclasts is weaker than the control group^[2]. Iguratimod (20 mg/kg i.p.) shows significantly increased survival in BALB/c mice that are vulnerable to endotoxemia, and attenuates TNFα release measured in serum isolated 90 min post-LPS administration in wild-type C57BL/6 mice^[3].

Clinical Trial

分子量

374.37

性状

Solid

Formula

C₁₇H₁₄N₂O₆S

CAS 号

123663-49-0

中文名称

艾拉莫德

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 : 33.33 mg/mL(89.03 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.6712 mL	13.3558 mL	26.7115 mL
5 mM	0.5342 mL	2.6712 mL	5.3423 mL
10 mM	0.2671 mL	1.3356 mL	2.6712 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% (20%SBE-β-CDin saline)
Solubility: 2.5 mg/mL (6.68 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.68 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 μL20% 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

*以上所有助溶剂都可在本网站选购。