西奈芬净

腺苷衍生物生物活性体外研究体内研究西奈芬净试剂级价格

西奈芬净

CAS号:58944-73-3
英文名:SINEFUNGIN
中文名:西奈芬净
CBNumber:CB9167377
分子式:C15H23N7O5
分子量:381.39
MOL File:58944-73-3.mol

西奈芬净化学性质

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
形态 :powder
酸度系数(pKa) :pKa (66% DMF): 2.9, 3.9, 8.9, 10.2(at 25℃)
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.

安全信息

危险品标志 :Xn
危险类别码 :22
安全说明 :36
WGK Germany :3
RTECS号 :HE3140000
海关编码 :29419090
毒性 :LD50 s.c. in mice: 185 mg/kg (Hamill, Hoehn, J. Antibiot.)

西奈芬净性质、用途与生产工艺

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.