204326-43-2
中文名稱(chēng)
4H-8-BROMO-1,2,4-OXADIAZOLO(3,4-D)BENZ(B)(1,4)OXAZIN-1-ONE
英文名稱(chēng)
NS-2028
CAS
204326-43-2
分子式
C9H5BrN2O3
分子量
269.05
MOL 文件
204326-43-2.mol
204326-43-2 結(jié)構(gòu)式
基本信息
中文別名
8-溴-1H,4H-[1,2,4]惡二唑并[3,4-C][1,4]苯并惡嗪-1-酮 英文別名
NS-2028NS 2028 - CAS 204326-43-2 - Calbiochem
4-H-BROMO-1,2,4-OXADIAZOLE(3,4-ALPHA)BENZ(B)OXAZIN-1-ONE
4H-8-BROMO-1,2,4-OXADIAZOLO(3,4-D)BENZ(B)(1,4)OXAZIN-1-ONE
4H-8-BROMO-1,2,4-OXADIAZOLO(3,4-D)BENZO(B)(1,4)OXAZIN-1-ONE
8-bromo-4~{H}-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one
8-Bromo-1H,4H-[1,2,4]Oxadiazolo[3,4-c][1,4]Benzoxazin-1-One
1H,4H-[1,2,4]Oxadiazolo[3,4-c][1,4]benzoxazin-1-one, 8-bromo-
8-BROMO-4H-2,5-DIOXA-3,9B-DIAZA CYCLOPENTA[A]NAPHTHALEN-1-ONE
物理化學(xué)性質(zhì)
熔點(diǎn)160～170℃
沸點(diǎn)353.8±52.0 °C(Predicted)
密度2.06±0.1 g/cm3(Predicted)
儲(chǔ)存條件+2C to +8C
溶解度DMSO: 13 mg/mL
溶解度在DMSO中的溶解度為13 毫克/毫升
酸度系數(shù)(pKa)-1.18±0.20(Predicted)
形態(tài)solid
顏色white
常見(jiàn)問(wèn)題列表
生物活性
NS-2028 是一種高選擇性可溶性鳥(niǎo)苷酸環(huán)化酶 (sGC) 抑制劑, 其 basal 和 NO 刺激的酶活性的 IC50 值分別為 30 nM 和 200 nM。NS-2028 抑制小鼠小腦勻漿和神經(jīng)元 NO 合酶中的可溶性鳥(niǎo)苷酸環(huán)化酶活性, IC50值分別為17 nM和20 nM。NS-2028 抑制 3-嗎啉代-sydnonimine (SIN-1) 在人培養(yǎng)的臍靜脈內(nèi)皮細(xì)胞中形成環(huán)狀GMP，IC50 值為30 nM。NS-2028 常用于一氧化氮信號(hào)通路的研究，它完全抑制非血管平滑肌中 NO 依賴(lài)性松弛反應(yīng) (1μM)。NS-2028 可降低血管內(nèi)皮生長(zhǎng)因子誘導(dǎo)的血管生成和通透性。靶點(diǎn)
IC50: 30 nM (soluble Guanylyl Cyclase sGC)
體外研究
NS-2028 (10 μM; 24 hours) inhibits 25% cell number in comparation with those grown in the presence of vehicle. NS-2028 (10 μM; 30 mins) attenuates VEGF-induced EC migration by inhibiting p38 MAPK activation.
Cell Proliferation Assay
| Cell Line: | HUVEC cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased cell numbers in culture. |
Western Blot Analysis
| Cell Line: | HUVEC cells |
| Concentration: | 10 μM |
| Incubation Time: | 30 mins |
| Result: | Attenuated VEGF-enhanced p38 phosphorylation. |
體內(nèi)研究
NS-2028 (Deliver orally; 1 g/L; 8 days) exhibits a significant reduction of new vessel formation in the avascular rabbit cornea in response to VEGF pellet implants.
| Animal Model: | Rabbit |
| Dosage: | 1 g/L |
| Administration: | Deliver orally; 1g/L; 8 days |
| Result: | Inhibits VEGF-induced angiogenesis in vivo. |