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.

Product information

CAS Number: 917909-71-8

Molecular Weight: 293.32

Formula: C16H15N5O

Synonym:

BIT-225

Chemical Name: N-carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide

Smiles: CN1C=C(C=N1)C1=CC=CC2=CC(=CC=C21)C(=O)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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

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. 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.

Products are for research use only. Not for human use.