SML3760

TFMT

≥98% (HPLC)

• Sinonimo/i: (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
• Formula empirica (notazione di Hill): C₁₂H₁₃F₃N₄O₄
• Numero CAS: 1854086-05-7
• Peso molecolare: 334.25
• Codice UNSPSC: 51111800
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: powder
• Colore: white to beige
• Solubilità: DMSO: 2 mg/mL, clear
• Temperatura di conservazione: -10 to -25°C

Descrizione

Azioni biochim/fisiol

SAM-binding pocket-targeting methyltransferase MTr1 inhibitor with anti-influenza efficacy in vitro and in vivo.

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).