GW274150 phosphate

产品编号 T11518Cas号 438542-15-5

别名

GW274150 phosphate is a selective, orally active, and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50: 2.19 μM; Kd: 40 nM) and rat iNOS (ED50: 1.15 μM).

GW274150 phosphate

产品编号 T11518Cas号 438542-15-5

GW274150 phosphate is a selective, orally active, and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50: 2.19 μM; Kd: 40 nM) and rat iNOS (ED50: 1.15 μM).

规格	价格	库存
2 mg	¥ 447	5日内发货
5 mg	¥ 747	5日内发货
10 mg	¥ 1,460	5日内发货
100 mg	¥ 6,650	8-10周

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产品介绍

生物活性

产品描述	GW274150 phosphate is a selective, orally active, and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50: 2.19 μM; Kd: 40 nM) and rat iNOS (ED50: 1.15 μM).
靶点活性	eNOS (human):544 μM (Kd)
体外活性	GW274150 is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively.GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50 values of 0.2±0.04 μM.
体内活性	GW274150 phosphate (oral adminstration; 30 mg/kg; twice daily; 7 days) leads to significant neuroprotection, however, it displays a bell-shaped neuroprotective profile, being ineffective at high doses in 6-OHDA rat model of Parkinson disease (PD).GW274150 phosphate is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2-, NO3- levels 14 h after single intraperitoneal dose (ED50=3 mg/kg).GW274150 phosphate (intraperitoneal injection;?2.5, 5, and 10 mg/kg;?before carrageenan injection) reduces the degree of lung injury induced by carrageenan in a dose-related fashion.?Oedema formation and PMNs infiltration in the pleural cavity are also significantly attenuated in a dose‐related manner in rats.

化学信息

分子量	317.3
分子式	C₈H₂₀N₃O₆PS
CAS No.	438542-15-5

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

H2O: 100 mg/mL (315.16 mM), Sonication is recommended.

溶液配制表

H2O

	1mg	5mg	10mg	50mg
1 mM	3.1516 mL	15.7580 mL	31.5159 mL	157.5796 mL
5 mM	0.6303 mL	3.1516 mL	6.3032 mL	31.5159 mL
10 mM	0.3152 mL	1.5758 mL	3.1516 mL	15.7580 mL
20 mM	0.1576 mL	0.7879 mL	1.5758 mL	7.8790 mL
50 mM	0.0630 mL	0.3152 mL	0.6303 mL	3.1516 mL
100 mM	0.0315 mL	0.1576 mL	0.3152 mL	1.5758 mL