58944-73-3
中文名称
西奈芬净
英文名称
SINEFUNGIN
CAS
58944-73-3
分子式
C15H23N7O5
分子量
381.39
MOL 文件
58944-73-3.mol
更新日期
2024/08/30 13:22:03
58944-73-3 结构式
基本信息
中文别名
西奈芬近西奈芬净
西奈芬净/D-GLYCERO-A-L-TALO-DECOFURANURONIC ACID,6,9-DIAMINO-1-(6-AMINO-9H-PURIN-9-YL)-1,5,6,7,8,9-HEXADEOXY-
英文别名
SFA-9145
rp32232
32232RP
SINEFUNGIN
SCF from rat
Steel Factor
compound57926
A 9145, RP 32232
ANTIBIOTIC A-9145
所属类别
生物化工：抑制剂物理化学性质
比旋光度D25 -2.61° (c = 5 in water); D23 +12 ±2° (c = 0.227 in water)
沸点783.2±70.0 °C(Predicted)
密度1.91±0.1 g/cm3(Predicted)
储存条件2-8°C
溶解度H2O: soluble
酸度系数(pKa)pKa (66% DMF): 2.9, 3.9, 8.9, 10.2(at 25℃)
形态powder
颜色white to yellow
稳定性Stable for 2 years from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 1 month.
安全数据
警示词警告
危险性描述H302-H315-H319-H335
危险品标志Xn
危险类别码22
安全说明36
WGK Germany3
RTECS号HE3140000
海关编码29419090
毒性LD50 s.c. in mice: 185 mg/kg (Hamill, Hoehn, J. Antibiot.)
常见问题列表
腺苷衍生物
西奈芬净（9，sinefungin）是一种腺苷衍生物，属于泛甲基转移酶抑制剂，最初作为一种潜在的抗真菌药物从灰质链霉菌中分离出来。Hercik 等报道了西奈芬净与ZIKV甲基转移酶所形成配合物的晶体结构。SAM 为MTase 的天然底物，西奈芬净是其竞争性抑制剂。 西奈芬净与GTP 和GDP 类似物相结合，可能增强这些类似物对酶的亲和力，从而得到更好的选择性和对ZIKV 复制更强的抑制作用。然而，西奈芬净作为抗寄生虫剂在犬和山羊上进行实验时，被发现具有毒性，阻碍了其临床应用。生物活性
Sinefungin是病毒粒子mRNA (鸟嘌呤-7-)-甲基转移酶、 mRNA (核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。Sinefungin 是一种 SET7/9 抑制剂，通过抑制H3K4甲基化来改善肾纤维化。体外研究
Sinefungin (0.5 or 1.0 μg/mL, 60 minutes) ameliorates the TGF-β1-induced increase of α-SMA and inhibits the upregulation of histone H3K4 monomethylation in renal epithelial cells and renal fibroblast cells.
Western Blot Analysis
| Cell Line: | Renal epithelial cells. |
| Concentration: | 0.5 or 1.0 μg/mL. |
| Incubation Time: | Pretreatment 60 minutes before TGF-β1 (10 ng/mL). |
| Result: | Significantly reduced TGF-β1-inducedα-SMA protein expression and inhibited H3K4me1 in a dose-dependent manner in both NRK-52E and NRK-49F cells. |
体内研究
Sinefungin (10 mg/kg, per day immediately after UUO) ameliorates renal fibrosis in obstructive nephropathy.
| Animal Model: | Male C57BL/6J mice (8 weeks of age). |
| Dosage: | 10 mg/kg |
| Administration: | Administered intraperitoneally per day immediately after UUO (prepared as a suspension in distilled water and 0.9% NaCl solution). |
| Result: |
Inhibited α-SMA protein expression.
Ameliorated those (α-SMA, FSP-1, collagen 1, collagen 3) both at 3 and 7 days after UUO. |