BIT225 | BIT-225 | CAS#917909-71-8 | NCp7 zinc finger inhibitor

BIT225
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526920

CAS#: 917909-71-8

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.

Chemical Structure

BIT225

CAS# 917909-71-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526920
Name: BIT225
CAS#: 917909-71-8
Chemical Formula: C16H15N5O
Exact Mass: 293.13
Molecular Weight: 293.330
Elemental Analysis: C, 65.52; H, 5.15; N, 23.88; O, 5.45

Price and Availability

Size	Price	Availability
1mg	USD 65	Ready to ship
5mg	USD 150	Ready to ship
10mg	USD 250	Ready to ship
25mg	USD 450	Ready to ship
50mg	USD 750	Ready to ship
100mg	USD 1350	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: BIT-225; BIT 225; BIT225.

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

InChi Key: WVROWPPEIMRGAB-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(C1=CC=C2C(C3=CN(C)N=C3)=CC=CC2=C1)NC(N)=N

Appearance: Solid powder

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

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.

Storage Condition: 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

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot# S21S11C23

QC Data:

View QC data: current batch, Lot# S21S11C23

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	BIT-225 is a NCp7 zinc finger inhibitor.
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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	0.0	0.00

Preparing Stock Solutions

The following data is based on the product molecular weight 293.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. 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. PMID: 20156486. 2. 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. PMID: 26858771; PMCID: PMC4745167.
In vitro protocol:	1. 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. PMID: 20156486. 2. 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. PMID: 26858771; PMCID: PMC4745167.
In vivo protocol:	TBD

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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.

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