58944-73-3
中文名稱
西奈芬凈
英文名稱
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
2024/12/23 09:09:17
58944-73-3 結(jié)構(gòu)式
基本信息
中文別名
西奈芬近西奈芬凈
西奈芬凈/D-GLYCERO-A-L-TALO-DECOFURANURONIC ACID,6,9-DIAMINO-1-(6-AMINO-9H-PURIN-9-YL)-1,5,6,7,8,9-HEXADEOXY-
英文別名
SFA-9145
rp32232
32232RP
SINEFUNGIN
SCF from rat
Steel Factor
compound57926
A 9145, RP 32232
ANTIBIOTIC A-9145
所屬類別
生物化工：抑制劑物理化學性質(zhì)
比旋光度D25 -2.61° (c = 5 in water); D23 +12 ±2° (c = 0.227 in water)
沸點783.2±70.0 °C(Predicted)
密度1.91±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度H2O: soluble
酸度系數(shù)(pKa)pKa (66% DMF): 2.9, 3.9, 8.9, 10.2(at 25℃)
形態(tài)powder
顏色white to yellow
穩(wěn)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.
安全數(shù)據(jù)
警示詞警告
危險性描述H302-H315-H319-H335
危險品標志Xn
危險類別碼22
安全說明36
WGK Germany3
RTECS號HE3140000
海關(guān)編碼29419090
毒性LD50 s.c. in mice: 185 mg/kg (Hamill, Hoehn, J. Antibiot.)
常見問題列表
腺苷衍生物
西奈芬凈（9，sinefungin）是一種腺苷衍生物，屬于泛甲基轉(zhuǎn)移酶抑制劑，最初作為一種潛在的抗真菌藥物從灰質(zhì)鏈霉菌中分離出來。Hercik 等報道了西奈芬凈與ZIKV甲基轉(zhuǎn)移酶所形成配合物的晶體結(jié)構(gòu)。SAM 為MTase 的天然底物，西奈芬凈是其競爭性抑制劑。 西奈芬凈與GTP 和GDP 類似物相結(jié)合，可能增強這些類似物對酶的親和力，從而得到更好的選擇性和對ZIKV 復制更強的抑制作用。然而，西奈芬凈作為抗寄生蟲劑在犬和山羊上進行實驗時，被發(fā)現(xiàn)具有毒性，阻礙了其臨床應用。生物活性
Sinefungin是病毒粒子mRNA (鳥嘌呤-7-)-甲基轉(zhuǎn)移酶、 mRNA (核苷-2'-)-甲基轉(zhuǎn)移酶和病毒增殖的有效抑制劑。Sinefungin 是一種 SET7/9 抑制劑，通過抑制H3K4甲基化來改善腎纖維化。體外研究
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. |
體內(nèi)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. |