Cellagen Technology LLC
 
작성일 : 13-07-19
[Cellagen Technology LLC] Current top sellers & new products of CellagenTech
J-147 / StemRegenin1 (SR1) / Y-27632 / TAK-875 / T-705 (Favipiravir) / PQ401
 
Current top sellers & new products of Cellagen Technology
  
 
Current top sellers
 
1st Product Name: J147
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J147 was discovered based upon efficacy in multiple cell culture models of age-associated pathologies rather than
exclusively amyloid metabolism. It is an exceptionally potent, orally active and broadly neuroprotective compound has the
ability to enhance memory in normal animals as well as to prevent memory deficits in Alzheimer’s disease (AD) transgenic
mice. The neurotrophic and memory-enhancing activities of J147 are associated with an increase in brain derived
neurotrophic factor (BDNF) levels and the expression of BDNF responsive proteins, the enhancement of LTP, the
preservation of synaptic protein, the reduction of amyloid plaques, etc. These pleiotrophic effects of a single molecule
suggest that J147 has potential for the treatment of AD.
 
Details
Chemical Formula:
 
C18H17F3IN2O2
CAS No.:
 
1146963-51-0
Molecular weight:
 
350.33
Purity:
> 98%
Appearance:
 
Yellow solid
Chemical name:
 
 (E)-N-(2,4-dimethylphenyl)-2,2,2-trifluoro-N'-(3-methoxybenzylidene)acetohydrazide
Solubility:
 
Up to 50 mM in DMSO
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
Reference
1. Qi Chen, et al. A novel neurotrophic drug for cognitive enhancement and Alzheimer's disease. PLoS One (2011),
   6(12), e27865.
 
 
2nd Product Name: StemRegenin1 (SR1)
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The compound StemRegenin 1 (SR1) is a selective, cell permeable, small molecule that promotes the self-renewal of
human hematopoietic stem cells in culture. SR1 is an antagonist of the aryl hydrocarbon receptor.
 
SR1 is the first small molecule that promotes robust expansion/self-renewal of human CD34+ peripheral blood and cord
blood hematopoietic stem cells (HSCs). Culture of HSCs with SR1 led to a 50-fold increase in cells expressing CD34 and a
17-fold increase in cells that retain the ability to engraft immunodeficient mice. SR1 can be potentially used for ex vivo
expansion of normal HSCs or leukemic stem/progenitor cells.
 
Details
Chemical Formula:
 
C24H23N5OS
CAS No.:
 
1227633-49-9
Molecular weight:
 
429.54
Purity:
> 98%
Appearance:
 
White solid
Chemical name:
 
 4-(2-((2-(benzo[b]thiophen-3-yl)-9-isopropyl-9H-purin-6-yl)amino)ethyl)phenol
Solubility:
 
Up to 35 mM in DMSO
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
1.  Anthony E. Boitano et al. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic
   Stem Cells. Science 10 September 2010: 1345-1348.
2. Smith G.H. et al. Identification of a high-affinity ligand that exhibits complete aryl hydrocarbon receptor antagonism.
   J Phar Exp Therap. 338 2011: 318-327
 
 
3rd Product Name: Y-27632
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Y-27632 is widely used as a specific inhibitor of the Rho-associated coiled-coil forming protein serine/threonine kinase
(ROCK) family. It has been found to prevent dissociation-induced apoptosis in human embryonic stem cells and enhance
the survival and cloning efficiency of dissociated hES cells without affecting their self-renewal properties or pluripotency.
Y-27632 can also enhance survival during the transplantation of ES cell-derived neural precursors.
 
Details
Chemical Formula:
 
C32H31BrN2O2
CAS No.:
 
146986-50-7
Molecular weight:
 
329.27
Purity:
> 98%
Appearance:
 
White solid
Chemical name:
 
 (1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide
Solubility:
 
Up to 100 mM in DMSO
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
1. Ishizaki, T. et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol
   (2000) 57: 976-983.
2. Koyanagi et al. Inhibition of the Rho/ROCK pathway reduces apoptosis during transplantation of embryonic stem
   cell-derived neural precursors. J. Neurosci Res (2008) 86: 270-280.
3. Watanabe et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells. Nat Biotech (2007)
   25: 681-686.   
 
 
4th Product Name: TAK-875
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TAK-875 is an orally-available, benzofuran-based, agonist of GPR40 for the potential treament of Type 2 diabetes mellitus,
with an human EC50 of 0.014 uM in a FLIPR assay. It has high selectivity over GPR41, GPR43, and GPR120, with EC50s all
greater than 10 uM. [1] Oral dosing (0.3-3 mg/kg) of TAK-875 in a glucose intolerance test in female Wistar rats reduced
blood glucose excursion. Insulin secretion was increased during an oral glucose tolerance test.
 
TAK-875 was shown to activate the Gqa-mediated signalling pathway in pancreatic b-cells. Prolonged agonist stimulation by TAK-875 revealed no evidence of b-cell dysfunction or toxicity, nor does it cause a induction of a marker of apoptosis in
pancreatic b-cells. [2]
 
Details
Chemical Formula:
 
C29H32O7S.1/2H2O
CAS No.:
 
1000413-72-8
Molecular weight:
 
533.63
Purity:
> 98%
Appearance:
 
White
Chemical name:
 
 [(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-
dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate
Solubility:
 
Up to 100 mM in DMSO
Synonyms:
 
TAK-875, TAK875
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
1. Negoro et al., ACS Med. Chem. Lett. 2010, 1, 290-294.
2. Tsujihata et al., TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist,
   enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2
   diabetic rats. J. Pharmacol. Exp. Ther. 2011, 339(1), 228-237. Pubmed ID: 21752941   
 
 
New products
 
Product Name: T-705 (Favipiravir)
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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:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
References
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: PQ401
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PQ401 is a diarylurea-based inhibitor of IGF-1R, inhibiting autophosphorylation in MCF-7 cells and the IGF-1R isolated
kinase domain at IC50s of 12 uM and < 1 uM, respectively. In IGF-1R stimulated MCF-7 cells, PQ401 was more effective at
an IC50 of 6 uM. In MCF-7 cells IGF-1-mediated signaling is decreased by way of the Akt antiapoptotic pathway. Prolonged incubation with PQ401 induces a dose-dependent increase in caspase activation. (1)
 
Details
Chemical Formula:
 
C18H16CIN3O2
CAS No.:
 
196868-63-0
Molecular weight:
 
341.79
Purity:
> 98%
Appearance:
 
White
Chemical name:
 
 N-(5-Chloro-2-methoxyphenyl)-N'-(2-methylquinolin-4-yl)urea
Solubility:
 
Up to 50 mM in DMSO
Synonyms:
 
PQ401, PQ-401
Storage:
Store solid powder at 4oC, or store DMSO solution at -20oC
 
Reference
1. Gable et al., Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast
   cancer cell growth. Mol. Cancer Ther. 2006, 5, 1079-1086. Pubmed ID: 16648580
 
 
Ordering information
 
Catalog No.
Product Name
Size
C5147-2
J-147
2mg, 10mg & 50mg
C7710-1
StemRegenin1 (SR1)
1mg, 5mg & 25mg
C9127-2
Y-27632
2mg, 10mg & 50mg
C8875-2
TAK-875
2mg, 10mg & 50mg
C8705-5
T-705 (Favipiravir)
5mg, 25mg & 100mg
C7740-5
PQ401
5mg, 25mg & 100mg
 
 
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