BIT225

• CAS: 917909-71-8
• Catalog Number: ACM917909718
• Category: Inhibitors
• Molecular Weight: 293.33
• Molecular Formula: C16H15N5O
• Description: BIT-225 is a NCp7 zinc finger inhibitor potentially for the treatment of HCV infection and HIV infection. BIT225 inhibits HIV-1 replication in myeloid dendritic cells. BIT225, inhibits bovine viral diarrhea virus in vitro and shows synergism with recombinant interferon-alpha-2b and nucleoside analogues. BIT225 against HIV-1 release from human macrophages.
• Synonyms: BIT-225; BIT 225; BIT225
• IUPAC Name: N-carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide
• Canonical SMILES: O=C(C1=CC=C2C(C3=CN(C)N=C3)=CC=CC2=C1)NC(N)=N
• InChI: InChI=1S/C16H15N5O/c1-21-9-12(8-19-21)13-4-2-3-10-7-11(5-6-14(10)13)15(22)20-16(17)18/h2-9H,1H3,(H4,17,18,20,22)
• InChI Key: WVROWPPEIMRGAB-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: BIT-225 is a NCp7 zinc finger inhibitor.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 65.52; H, 5.15; N, 23.88; O, 5.45
• Exact Mass: 293.1277
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: The anti-HIV-1 activity of BIT225 was evaluated in vitro within MDDC (monocyte-derived DC) alone and in co-cultures with activated CD4(+) T cells to examine the effect of the drug on HIV-1 transfer. Antiviral activity was determined by measuring HIV-1 reverse transcriptase activity in the culture supernatant of BIT225 treated and DMSO control cultures. Despite expected donor-donor variation in the level of HIV-1 infection of the MDDC, the antiviral activity of BIT225 was evident in all three donors compared to the DMSO controls (DMSO v BIT225 at Day 14, n = 2, p = 0.12). When represented as a mean (±SE) percentage of viral inhibition compared to the DMSO controls, the anti-HIV-1 activity of BIT225 increased over time with inhibition at 28.0 % (±87.9), 55.3 % (±12.2), 67.3 % (±11.0), and 74.5 % (±0.6) for days 8, 10, 11/12 and 14 respectively. In the co-cultures, a single BIT225 treatment of the infected MDDC resulted in a reduction in the transfer of HIV-1 from the MDDC to the uninfected CD4+ T cells when the source of HIV-1 was from de novo viral production, cis transfer. The antiviral effect of BIT225 increased over time following MDDC infection, such that increased exposure to BIT225 resulted in a decreased virus burden within the MDDC, leading to a reduction in HIV-1 transfer to the more permissive CD4+ T cell (DMSO v BIT225 at Day 12, n = 2, p = 0.12). These findings suggest a potential role for BIT225 in reducing HIV-1 production and preventing viral dissemination.; Reference: AIDS Res Ther. 2016 Feb 8;13:7. https://pubmed.ncbi.nlm.nih.gov/26858771/
• In Vivo Activity: TBD
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).