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438542-15-5

中文名稱 GW274150 PHOSPHATE
英文名稱 GW274150 phosphate
CAS 438542-15-5
分子式 C8H20N3O6PS
分子量 317.3
MOL 文件 438542-15-5.mol
更新日期 2024/12/16 15:20:14
438542-15-5 結(jié)構(gòu)式 438542-15-5 結(jié)構(gòu)式

基本信息

中文別名
GW274150 PHOSPHATE
英文別名
GW274150 phosphate

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
形態(tài)Solid
顏色White to off-white
水溶解性Water: 100 mg/mL (315.16 mM)
GW274150 PHOSPHATE價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-12119AGW274150 PHOSPHATE
GW274150 phosphate
438542-15-55mg900元
2024/11/08HY-12119AGW274150 PHOSPHATE
GW274150 phosphate
438542-15-510mM * 1mLin Water990元
2024/11/08HY-12119AGW274150 PHOSPHATE
GW274150 phosphate
438542-15-510mg1500元

常見問題列表

生物活性
GW274150 phosphate 是一種有效的,選擇性的,口服活性的 NADPH 依賴型人誘導(dǎo)型一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠 (iNOS) 抑制劑。GW274150 phosphate 對(duì)人和大鼠內(nèi)皮一氧化氮合酶 (eNOS) 和神經(jīng)元一氧化氮合酶 (nNOS) 均顯示較低效力。GW274150 phosphate 在急性肺損傷炎癥模型中發(fā)揮保護(hù)作用。
靶點(diǎn)

Kd: 40 nM (iNOS)IC50: 2.19 μM (human iNOS); 544 μM (human eNOS); 177 μM (human nNOS)ED50: 1.15 μM (rat iNOS); 252 μM (rat nNOS)

體外研究

GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC 50 values of 0.2±0.04 μM.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.

體內(nèi)研究

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 (ED 50 =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.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).

Animal Model: SD rat
Dosage: 2.5, 5 and 10 mg/kg
Administration: Intraperitoneal injection 5 min before carrageenan injection
Result: Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
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