BIT225
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.
For research use only. We do not sell to patients.
Chemical Information
| Name | BIT225 |
|---|---|
| Iupac Chemical Name | N-carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide |
| Synonyms | BIT-225; BIT 225; BIT225. |
| Molecular Formula | C16H15N5O |
| Molecular Weight | 293.32 |
| Smile | O=C(C1=CC=C2C(C3=CN(C)N=C3)=CC=CC2=C1)NC(N)=N |
| InChiKey | WVROWPPEIMRGAB-UHFFFAOYSA-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) |
| CAS Number | 917909-71-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | 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. |
| HS Code |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Khoury G, Ewart G, Luscombe C, Miller M, Wilkinson J. The antiviral compound BIT225 inhibits HIV-1 replication in myeloid dendritic cells. AIDS Res Ther. 2016 Feb 8;13:7. doi: 10.1186/s12981-016-0093-z. eCollection 2016. PubMed PMID: 26858771; PubMed Central PMCID: PMC4745167.
2: Wilkinson J, Ewart G, Luscombe C, McBride K, Ratanasuwan W, Miller M, Murphy RL. A Phase 1b/2a study of the safety, pharmacokinetics and antiviral activity of BIT225 in patients with HIV-1 infection. J Antimicrob Chemother. 2016 Mar;71(3):731-8. doi: 10.1093/jac/dkv389. Epub 2015 Nov 29. PubMed PMID: 26620101.
3: Mathew S, Fatima K, Fatmi MQ, Archunan G, Ilyas M, Begum N, Azhar E, Damanhouri G, Qadri I. Computational Docking Study of p7 Ion Channel from HCV Genotype 3 and Genotype 4 and Its Interaction with Natural Compounds. PLoS One. 2015 Jun 1;10(6):e0126510. doi: 10.1371/journal.pone.0126510. eCollection 2015. PubMed PMID: 26030803; PubMed Central PMCID: PMC4451521.
4: Tietjen I, Ntie-Kang F, Mwimanzi P, Onguéné PA, Scull MA, Idowu TO, Ogundaini AO, Meva'a LM, Abegaz BM, Rice CM, Andrae-Marobela K, Brockman MA, Brumme ZL, Fedida D. Screening of the Pan-African natural product library identifies ixoratannin A-2 and boldine as novel HIV-1 inhibitors. PLoS One. 2015 Apr 1;10(4):e0121099. doi: 10.1371/journal.pone.0121099. eCollection 2015. PubMed PMID: 25830320; PubMed Central PMCID: PMC4382154.
5: Bichmann L, Wang YT, Fischer WB. Docking assay of small molecule antivirals to p7 of HCV. Comput Biol Chem. 2014 Nov 13;53PB:308-317. doi: 10.1016/j.compbiolchem.2014.11.001. [Epub ahead of print] PubMed PMID: 25462337.
6: Meredith LW, Zitzmann N, McKeating JA. Differential effect of p7 inhibitors on hepatitis C virus cell-to-cell transmission. Antiviral Res. 2013 Dec;100(3):636-9. doi: 10.1016/j.antiviral.2013.10.006. Epub 2013 Oct 21. PubMed PMID: 24157306; PubMed Central PMCID: PMC3851685.
7: Wang YT, Hsu HJ, Fischer WB. Computational modeling of the p7 monomer from HCV and its interaction with small molecule drugs. Springerplus. 2013 Jul 18;2:324. doi: 10.1186/2193-1801-2-324. eCollection 2013. PubMed PMID: 23961398; PubMed Central PMCID: PMC3724979.
8: Gazina EV, Petrou S. Viral targets of acylguanidines. Drug Discov Today. 2012 Sep;17(17-18):1039-43. doi: 10.1016/j.drudis.2012.05.002. Epub 2012 May 8. Review. PubMed PMID: 22580299.
9: Kuhl BD, Cheng V, Donahue DA, Sloan RD, Liang C, Wilkinson J, Wainberg MA. The HIV-1 Vpu viroporin inhibitor BIT225 does not affect Vpu-mediated tetherin antagonism. PLoS One. 2011;6(11):e27660. doi: 10.1371/journal.pone.0027660. Epub 2011 Nov 14. PubMed PMID: 22110710; PubMed Central PMCID: PMC3215742.
10: Luscombe CA, Huang Z, Murray MG, Miller M, Wilkinson J, Ewart GD. A novel Hepatitis C virus p7 ion channel inhibitor, BIT225, inhibits bovine viral diarrhea virus in vitro and shows synergism with recombinant interferon-alpha-2b and nucleoside analogues. Antiviral Res. 2010 May;86(2):144-53. doi: 10.1016/j.antiviral.2010.02.312. Epub 2010 Feb 13. PubMed PMID: 20156486.
11: Khoury G, Ewart G, Luscombe C, Miller M, Wilkinson J. Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. Antimicrob Agents Chemother. 2010 Feb;54(2):835-45. doi: 10.1128/AAC.01308-09. Epub 2009 Dec 7. PubMed PMID: 19995924; PubMed Central PMCID: PMC2812169.
Chemical Structure
