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Merck

SML3760

TFMT

≥98% (HPLC)

别名:

(2R,3R,4S,5R)-2-(4-Amino-5-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol, 5-Trifluoromethyl-tubercidin, 7-β-D-Ribofuranosyl-5-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, Trifluoromethyl-tubercidin

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About This Item

经验公式(希尔记法):
C12H13F3N4O4
分子量:
334.25
分類程式碼代碼:
51111800
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

-10 to -25°C

生化/生理作用

Trifluoromethyl-tubercidin (TFMT) is a SAM-binding pocket-targeting methyltransferase (MTase) MTr1 inhibitor that impedes the maturation of host cap RNAs and their binding with influenza viral polymerase. TFMT selectively inhibits influenza A&B (IAV & IBV), but not Hazara virus (HAZV) or soft tick bunyavirus (STBV), replication in epithelial cultures (IAV IC50 = 300 nM/human A549, 7.7 μM/murine LA-4) with little toxicity (up to 1 mM; A549 cells). TFMT suppresses IAV replication in mice in vivo (2 mg/kg intranasally on day 0 and day 1 of IAV infection) and synergizes with anti-influenza drugs baloxavir marboxil (BXM; endonuclease inhibitor) and oseltamivir (neuraminidase inhibitor).

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Inhibition of cellular RNA methyltransferase abrogates influenza virus capping and replication
Science (New York, N.Y.), 379(6632), 586-591 (2023)

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