MPO-IN-1|cas:2471981-21-0|西域试剂

MPO-IN-1,99.02%

产品编号：Bellancom-139915| CAS NO：2471981-21-0| 分子式：C₂₄H₂₁ClN₄| 分子量：400.90

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-139915		￥5100.00	杭州北京（现货）
Bellancom-139915		￥8200.00	杭州北京（现货）

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MPO-IN-1

产品介绍

MPO-IN-1 是一种有效的, 具有口服活性的，不可逆的含有吲哚结构的髓过氧化物酶 (MPO) 抑制剂，对 MPO 和甲状腺过氧化物 (TPO) 的 IC₅₀ 值分别为 2.6 μM 和 5.3 μM。MPO-IN-1 在急性炎症小鼠模型中抑制 MPO 活性。

生物活性

MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC₅₀s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation.

体外研究

体内研究

MPO-IN-1 (compound 2) (5 and 90 mg/kg; p.o.; four hours post-Zymosan A administration) significantly reduces MPO activity in a mouse peritonitis model of acute inflammation.
Mouse pharmacokinetic parameter of MPO-IN-1.

Dose	V_ss (L/kg)	T_1/2 (h)	AUC_inf (nM•h) p.o.	C_max (nM) p.o.	PPB (%)	F (%)
1/10 mg/kg i.v./p.o.	9.8	2.6	2486	502	99.6	61

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

Animal Model:	Male C57BL/6J mice (mouse peritonitis model of acute inflammation)
Dosage:	5 and 90 mg/kg
Administration:	p.o. (four hours post-Zymosan A administration)
Result:	Resulted in a ~50% reduction in the MPO activity at 90 mg/kg.

体内研究

Dose	V_ss (L/kg)	T_1/2 (h)	AUC_inf (nM•h) p.o.	C_max (nM) p.o.	PPB (%)	F (%)
1/10 mg/kg i.v./p.o.	9.8	2.6	2486	502	99.6	61

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

Animal Model:	Male C57BL/6J mice (mouse peritonitis model of acute inflammation)
Dosage:	5 and 90 mg/kg
Administration:	p.o. (four hours post-Zymosan A administration)
Result:	Resulted in a ~50% reduction in the MPO activity at 90 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (498.88 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4944 mL	12.4719 mL	24.9439 mL
5 mM	0.4989 mL	2.4944 mL	4.9888 mL
10 mM	0.2494 mL	1.2472 mL	2.4944 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式