Disease Area, Infectious Disease IV
Product Name: T-705 (Favipiravir) l Anti-influenza compound (#C8705-5)
.png)
T-705 (Favipiravir) is an antiviral pyrazinecarboxamide-based, inhibitor of of the influenza virus with an EC90
of 1.3 to 7.7 uM (influenza A, H5N1). EC90 ranges for other influenza A subtypes are 0.19-1.3 uM, 0.063-1.9
uM, and 0.5-3.1 uM for H1N1, H2N2, and H3N2, respectively. T-705 also exhibits activity against type B and C
viruses, with EC90s of 0.25-0.57 uM and 0.19-0.36 uM, respectively. (1) Additionally, T-705 has broad activity
against arenavirus, bunyavirus, foot-and-mouth disease virus, and West Nile virus with EC50s ranging from 5
to 300 uM. (1)
Studies show that T-705 ribofuranosyl triphosphate is the active form of T-705 and acts like purines or purine
nucleosides in cells and does not inhibit DNA synthesis. (2)
|
Details
|
Chemical Formula:
|
|
C5H4FN3O2
|
|
CAS No.:
|
|
259793-96-9
|
|
Molecular weight:
|
|
157.1
|
|
Purity:
|
|
> 98%
|
|
Appearance:
|
|
off white
|
|
Chemical name:
|
|
6-fluoro-3-hydroxy-2-pyrazinecarboxamide
|
|
Solubility:
|
|
Up to 100 mM in DMSO
|
|
Synonyms:
|
|
T-705, T705, Favipiravir
|
|
Storage:
|
|
For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
|
1. Furuta et al., T-705 (favipiravir) and related compounds: Novel broad-spectrum inhibitors of RNA viral
infections. Antiviral Res. 2009, 82, 95-102. Pubmed ID: 19428599
2. Kiso et al., T-705 (favipiravir) activity against lethal H5N1 influenza A viruses. Proc. Natl. Acad. Sci. 2010,
107(2), 882-887. Pubmed ID: 20080770
|
Product Name: TMC114 (Darunavir) l HIV-1 protease inhibitor (#C8114-5)
.png)
Darunavir Ethanolate (TMC114), a phenylalanine mimic, is a potent inhibitor of HIV-1 protease with EC50
activity against the wild type IIIB strain of 4 nM and an average EC50 activity against mutant protease inhibitor
strains M1-M5 of 5 nM. [1] Furthermore, fof 150 protease inhibitor-resistant viruses tested, 75% were inhibited
by darunavir with a EC50 of
Darunavir exhibits no cytotoxicity at concentrations up to 100 uM and has been shown to be synergistic with
a variety of other protease inhibitors and reverse transcriptase inhibitors. [3]
|
Details
|
Chemical Formula:
|
|
C27H37N3O7S.C2H5OH
|
|
CAS No.:
|
|
635728-49-3
|
|
Molecular weight:
|
|
593.73
|
|
Purity:
|
|
> 98%
|
|
Appearance:
|
|
White
|
|
Chemical name:
|
|
N-[(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-
(phenylmethyl)propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl
ester compd. with ethanol
|
|
Solubility:
|
|
Up to 100 mM in DMSO
|
|
Synonyms:
|
|
TMC114, 635728-49-3, Darunavir Ethanolate, Darunavir, Prezista
|
|
Storage:
|
|
For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
|
References
1. Surleraux et al., Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor. J. Med.
Chem. 2005, 48, 1813-1822. Pubmed ID: 15771427
2. Molina et al., Darunavir (TMC114): a new HIV-1 protease inhibitor. Expert Opin. Pharmacother. 2007,
8(12), 1951-1964. Pubmed ID: 17696796
3. De Meyer et al., TMC114, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor Active against
Protease Inhibitor-Resistant Virsues, Including a Broad Range of Clinical Isolates. Antimicrob. Agents.
Chemother. 2005, 49(6), 2314-2321.
|
Product Name: TMC125 (Etravirine) | HIV-1 reverse transcriptase inhibitor (#C8125-5)
.png)
TMC125 is a nonnucleoside reverse transcriptase inhibitor with an EC50 of 1.4 to 4.3 nM for wild-type HIV-1.
Additionally, TMC125 is highly potent against a wide range of single-mutant and double-mutant NNRTI-
resistant HIV-1 strains, including L100I, K103N, Y181C, and L100I+K103N, at EC50s of 3, 1, 7, and 19 nM,
respectively. (1)
TMC125 is believed to have a high barrier to development of resistance in vitro based on multiplicity of
infection experiments which confirm a profile distinct from other reverse transcriptase inhibitors. (2)
|
Details
|
Chemical Formula:
|
|
C20H15BrN6O
|
|
CAS No.:
|
|
269055-15-4
|
|
Molecular weight:
|
|
435.28
|
|
Purity:
|
|
> 98%
|
|
Appearance:
|
|
White
|
|
Chemical name:
|
|
4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)pyrimidin-4-yl)oxy)-3,5-
dimethylbenzonitrile
|
|
Solubility:
|
|
Up to 50 mM in DMSO
|
|
Synonyms:
|
|
TMC125, TMC-125, Etravirine
|
|
Storage:
|
|
For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
|
References
1. Andries et al., TMC125, a Novel Next-Generation Nonnucleoside Reverse Transcriptase Inhibitor Active
against Nonnucleoside Reverse Transcriptase Inhibitor-Resistant Human Immunodeficiency Virus Type 1.
Antimicrob. Agents Chemother. 2004, 48(12), 4680-4686. Pubmed ID: 15561844
2. Vingerhoets et al., TMC125 Displays a High Genetic Barrier to the Development of Resistance: Evidence
from In Vitro Selection Experiments. J. Virol. 2005, 79(20), 12773-12782. Pubmed ID:16188980
|
Product Name: TMC207 (Bedaquiline) | ATP synthase inhibitor (#C8207)
.png)
Saquinavir is a decahydroisoquinoline-based, selective inhibitor of aspartic protease encoded by HIV with
an IC50 range of 0.5-6.0 nM and IC90 range of 6.0-30.0 nM. [1] Binding inhibition constants for saquinavir
against HIV-1 and HIV-2 are 0.12 nM and
Antiviral potency of saquinavir were shown in JM cells infected with HIV-1 strain GB8 with a IC50 of 2.5 nM.
[2] Similarly, and IC50 of 2 nM was obtained against HIV-1 (strain RF) in C8166 cells.
Saquinavir was shown to be a substrate for P-glycoprotein transporter protein, affecting intracellular
concentrations and bioavailability. [3]
|
Details
|
Chemical Formula:
|
|
C32H31BrN2O2
|
|
CAS No.:
|
|
843663-66-1
|
|
Molecular weight:
|
|
555.5
|
|
Purity:
|
|
> 98%
|
|
Appearance:
|
|
White
|
|
Chemical name:
|
|
(1R,2S)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-
yl)-1-phenylbutan-2-ol
|
|
Solubility:
|
|
Up to 2 mM in DMSO
|
|
Synonyms:
|
|
TMC207, TMC-207, Bedaquiline
|
|
Storage:
|
|
For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
|
References
1. Matteelli et al., TMC207: the first compoudn of a new class of potent anti-tuberculosis drugs. Future
Microbiol. 2010, 5(6), 849-858. Pubmed ID: 20521931
2. Rustomjee et al., Early Bactericidal Activity and Pharmacokinetics of the Diarylquinoline TMC207 in
Treatment of Pulmonary Tuberculosis. Antimicrob. Agents Chemother. 2008, 52(8), 2831-2835. Pubmed ID:
18505852
|
|