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VX-765 & other new products of Cellagen Technology

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VX-765 & other new products of Cellagen Technology
 
 
Product Name: VX-765
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VX-765 is an orally-available prodrug of VRT-043198, an inhibitor of interleukin-converting enzyme / caspase-1 subfamily
caspases. VRT-043198 shows Ki values of 0.8 nM and 100-fold selectivity over other non-ICE subfamily caspases.
VRT-043198 showed no significant activity towards trypsin or cathepsin B. (1)
VRT-043198 inhibits IL-1b release from both PBMCs and whole blood with IC50 values of 0.67 and 1.9 uM, respectively.
Additionally in stimulated PBMCs, VRT-043198 dose-dependently inhibited IL-1b, IL-18, and IFN-g, without affecting TNF-a
release. In a hypoxia-induced apoptosis assay employing the NT2 human neuroblastoma cell line, VRT-043198 did not
alter ischemia-induced apoptosis up to concentrations of 100 uM. (1)
According to Vertex's news release , VX-765 has been shown to inhibit acute seizures in preclinical models of acute
epilepsy and has shown activity in preclinical models of chronic epilepsy that do not respond to standard anti-epileptic
drugs. (2)
 
Details
Chemical Formula:
 
C24H33CIN4O6
CAS No.:
 
273404-37-8
Molecular weight:
 
509
Purity:
> 99%
Appearance:
 
White
Chemical name:
 
 (S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-
6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Solubility:
 
Up to 50 mM in DMSO
Synonyms:
 
VX-765, VX-765
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
Reference
1. Wannamaker et al., (S)-1-((S)-2-{[1-(4-Amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-
   2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an Orally Available Selective
   Interleukin (IL)-Converting Enzyme/ Caspase-1 Inhibitor, Exhibits Potent Anti-Inflammatory Activities by Inhibiting the
   Release of IL-1b and IL-18. J. Pharmacol. Exp. Ther. 2007, 321(2), 509-516. Pubmed ID: 17289835   
 
 
Product Name: Tolrestat
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Tolrestat is a thioamide-based inhibitor of aldose reductase with an IC50 activity of 35 nM. (1) Along with other similar
therapies, Tolrestat has implications in the treatment of diabetic complications, such as diabetic neuropathy, in a manner
independent of insulin-related control of blood glucose levels. (2)
In rat diabetes models, Tolrestat reduces sorbitol concentrations in the sciatic nerve and eye lens, as well as prevents
diabetic retinopathy, cateracts, thickening of the retinal basement membrane, and nerve dysfunction. Additionally,
Tolrestat reduces urinary albumin excretion. (3)
 
Details
Chemical Formula:
 
C16H14F3NO3S
CAS No.:
 
82964-04-3`
Molecular weight:
 
357.35
Purity:
> 98%
Appearance:
 
White
Chemical name:
 
 2-(6-methoxy-N-methyl-5-(trifluoromethyl)naphthalene-1-carbothioamido)acetic acid
Solubility:
 
Up to 22 mM in DMSO
Synonyms:
 
Tolrestat
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
Reference
1. Sestanj et al., N-[[5 -(Trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]-N-methylglycine (Tolrestat), a Potent,
   Orally Active Aldose Reductase Inhibitor. J. Med. Chem. 1984, 27, 255-256. Pubmed ID: 6422042   
2. Kador et al., Aldose Reductase Inhibitors: A Potential New Class of Agents for the Pharmacological Control of Certain
   Diabetic Complications. J. Med. Chem. 1985, 28(7), 841-849. Pubmed ID: 3925146
3. Fruncillo et al., Pharmacokinetics of the aldose reductase inhibitor tolrestat: Studies in healthy young and elderly male
   and female subjects and in subjects with diabetes. Clin. Pharmcol. Ther. 1996, 59(6), 602-613. Pubmed ID: 8681485
 
 
Product Name: TMC207 (Bedaquiline)
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TMC207 (Bedaquiline) is a diarylquinoline-based inhibitor of bacterial ATP synthase at nanomolar concentrations. In vitro
mycobacterial experiments show that TMC207 inhibits drug-sensitive and drug-resistant mycobacterial TB at an MIC range of 2 to 60 nM and an MIC50 of 30 ng/mL. Additionally TMC207 is broadly potent against many non-tuberculous
mycobacteria, with MICs of 6 to 500 nM. (1)
Studies show that TMC207 is orally-available and efficacious on a once-daily administration for patients with pulmonary
TB. No serious adverse events were observed. (2)
 
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 50 mM in DMSO
Synonyms:
 
TMC207, TMC-207, Bedaquiline
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
Reference
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   
 
 
Product Name: TMC125(Etravirine)
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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:
Store solid powder at 4oC, or store 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: RAD001 (Everolimus)
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RAD001 (Everolimus) is an orally-bioavailable, semi-synthetic compound with immunosuppressive activity. It has an IC50
against FKBP12 (FK506-binding protein 12) of 1.8-2.6 nM. Moreover, in an IL-6-dependent hybridoma clone, growth
factor-stimulated cell proliferation was measured at an IC50 of 0.2-1.4 nM. Immunosuppressant activity was measured
in a mouse lymphocyte reaction model and was determined to be 0.2-1.6 nM. In a Human T-cell clone model, its IC50
was 0.05-0.17 nM. (1)
Everolimus binds to FKBP12, thus forming a complex that inhibits mTOR activity and concomitantly reduces downstream
markers such as S6 ribosomal protein kinase (S6K1) and eukaryotic elongation factor 4E-binding protein (4EBP). (2)
Everolimus has been used in combination with agents such as Letrozole to inhibit proliferation and trigger apoptosis,
which has implications in therapies for hormone-dependent breast cancers. (3)
 
Details
Chemical Formula:
 
C53H83NO14
CAS No.:
 
159351-69-6
Molecular weight:
 
958.22
Purity:
> 98%
Appearance:
 
White
Chemical name:
 
 40-O-(2-hydroxyethyl) derivative of sirolimus
Solubility:
 
Up to 30 mM in DMSO
Synonyms:
 
RAD-001, RAD001, Everolimus
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
1. Nashan, B. et al., Review of the proliferation inhibitor everolimus. Expert Opin. Investig. Drugs. 2002, 11(12),
   1845-1857. Pubmed ID: 12457444
2. Atkins et al., Everolimus. Nat. Rev. Drug Disc. 2009, 8, 535-536. Pubmed ID: 19568281
3. Boulay et al., Dual Inhibition of mTOR and Estrogen Receptor Signaling In vitro Induces Cell Death inModels of Breast
   Cancer. Clin. Cancer Res. 2005, 11, 5319-5328. Pubmed ID: 16033851   
 
 
Product Name: PSI-6206 (RO2433)
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PSI-6206 (RO2433) is the unphosphorylated parent compound of triphosphate analog PSI-7409, which is a potent
inhibitor of the HCV NS5B RNA dependent RNA polymerase. The monophosphate form of PSI-6206 was shown to be
metabolized in primary human hepatocytes to its triphosphate analog PSI-7409. Furthermore, the phosphoramidate
prodrug of PSI-6206 monophosphate, PSI-7851, was developed. Alternatively, PSI-6130, an aminated analog of
PSI-6206 monophosphate, was also developed. (1,2,3)
PSI-7409, the triphosphate of PSI-6206 inhibits wild-type and S282T HCV RdRp with Ki values of 0.42 and 22 uM,
respectively. PSI-7851, the phosphoramidate of PSI-6206 monophosphate, showed an EC50 value of 1.62 uM for
inhibiting HCV RNA replication. (2)
 
Details
Chemical Formula:
 
C10H13FN2O5
CAS No.:
 
863329-66-2
Molecular weight:
 
260.22
Purity:
> 98%
Appearance:
 
Clear Crystal
Chemical name:
 
 (2'R)-2'-Deoxy-2'-fluoro-2'-methyluridine
Solubility:
 
Up to 100 mM in DMSO
Synonyms:
 
PSI-6206, RO-2433, PSI6206, RO2433
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
1. Rodriguez-Torres et al., Antiviral Activity, Pharmacokinetics, Safety, and Tolerability of PSI-7851, a Novel Nucleotide
   Polymerase Inhibitor for HCV, Following Single and 3 Day Multiple Ascending Oral Doses in Healthy Volunteers and
   Patients with Chronic HCV Infection. 60th AASLD Annual Meeting, 2009.
2. Murakami et al., The Mechanism of Action of b-D-2'-Deoxy-2'-Fluoro-2'-C-Methylcytidine Involves a Second Metabolic
   Pathway Leading to b-D-2'-Deoxy-2'-Fluoro-2'-C-Methyluridine 5'-Triphosphate, a Potent Inhibitor of the Hepatitis C
   Virus RNA-Dependent RNA Polymerase. Antimicrob. Agents. Chemother. 2008, 52(2), 458-464.
   Pubmed ID: 17999967
3. Ma et al., Characterization of the Metabolic Activation of Hepatitis C Virus Nucleoside Inhibitor b-D-2'-Deoxy-2'-fluoro-2'-
   C-methylcytidine (PSI-6130) and Identification of a Novel Active 5'-Triphosphate Species. J. Biol. Chem.
   2007, 282, 29812-29820. Pubmed ID: 17698842
 
 
Ordering information
 
Catalog No.
Product Name
Size
C8976-5
VX-765
5mg, 25mg & 100mg
C8657-5
Tolrestat
5mg, 25mg & 100mg
C8207-5
TMC207 (Bedaquiline)
5mg, 25mg & 100mg
C8125-5
TMC125 (Etravirine)
5mg, 25mg & 100mg
C7230-5
RAD001 (Everolimus)
5mg, 25mg & 100mg
C7620-2
PSI-6206 (RO2433)
2mg, 10mg & 50mg
 
 
 
 

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