Synonym
KP-1461; KP1461; KP 1461
IUPAC/Chemical Name
Carbamic acid, (5-(2-deoxy-beta-D-erythro-pentofuranosyl)-1,4,5,6-tetrahydro-4-oxo-1,3,5-triazin-2-yl)-, heptyl ester
InChi Key
SZWIAFVYPPMZML-YNEHKIRRSA-N
InChi Code
InChI=1S/C16H28N4O6/c1-2-3-4-5-6-7-25-16(24)19-14-17-10-20(15(23)18-14)13-8-11(22)12(9-21)26-13/h11-13,21-22H,2-10H2,1H3,(H2,17,18,19,23,24)/t11-,12+,13+/m0/s1
SMILES Code
O=C(OCCCCCCC)NC(NCN1[C@H]2C[C@@H]([C@@H](CO)O2)O)=NC1=O
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
>3 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
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
372.42
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 |
1: Hicks C, Clay P, Redfield R, Lalezari J, Liporace R, Schneider S, Sension M, McRae M, Laurent JP. Safety, tolerability, and efficacy of KP-1461 as monotherapy for 124 days in antiretroviral-experienced, HIV type 1-infected subjects. AIDS Res Hum Retroviruses. 2013 Feb;29(2):250-5. doi: 10.1089/AID.2012.0093. Epub 2012 Aug 27. PubMed PMID: 22738014; PubMed Central PMCID: PMC3552433.
2: Harris KS, Brabant W, Styrchak S, Gall A, Daifuku R. KP-1212/1461, a nucleoside designed for the treatment of HIV by viral mutagenesis. Antiviral Res. 2005 Jul;67(1):1-9. PubMed PMID: 15890415.
3: Becker S. New kind of antiretroviral, KP-1461; clinical trial recruiting. Interview with Stephen Becker, M.D. AIDS Treat News. 2007 Jul-Sep;(423):3-7. PubMed PMID: 18411488.
4: Mullins JI, Heath L, Hughes JP, Kicha J, Styrchak S, Wong KG, Rao U, Hansen A, Harris KS, Laurent JP, Li D, Simpson JH, Essigmann JM, Loeb LA, Parkins J. Mutation of HIV-1 genomes in a clinical population treated with the mutagenic nucleoside KP1461. PLoS One. 2011 Jan 14;6(1):e15135. doi: 10.1371/journal.pone.0015135. PubMed PMID: 21264288; PubMed Central PMCID: PMC3021505.
5: Novel anti-HIV agent enters Phase IIa clinical trial. Expert Rev Anti Infect Ther. 2007 Aug;5(4):540-1. PubMed PMID: 17678417.