Basic information Safety Supplier Related

SB-505124

Basic information Safety Supplier Related

SB-505124 Basic information

Product Name:
SB-505124
Synonyms:
  • TGF-β RI Kinase Inhibitor III - CAS 356559-13-2 - Calbiochem
  • TGF-β RI Kinase Inhibitor III
  • Pyridine, 2-[5-(1,3-benzodioxol-5-yl)-2-(1,1-diMethylethyl)-1H-iMidazol-4-yl]-6-Methyl-, Monohydrochloride
  • SB-505124 hydrochloride
  • SB-505124 HCl
  • TGF-β RI Kinase Inhibitor III
CAS:
356559-13-2
MF:
C20H22ClN3O2
MW:
371.87
Mol File:
356559-13-2.mol
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SB-505124 Chemical Properties

storage temp. 
2-8°C
solubility 
DMSO: 24 mg/mL
form 
solid
color 
yellow
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Safety Information

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
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SB-505124 Usage And Synthesis

Uses

TGF-beta RI Kinase Inhibitor III is an inhibitor of activin receptor-like kinase 4.

Biological Activity

sb505124 is a selective inhibitor of tgfβr for alk4, alk5 with ic50 value of 129 nm and 47 nm [1].anaplastic lymphoma kinase (alk) gets involved in the development of the brain and influence specific neurons in the nervous system.sb505124 is a reversible atp competitive inhibitor of alk4 and alk5. incubation of the alk5 with high concentrations of sb505124, followed by dilution to a sub-ic50 concentration resulted in no effect of downstream smad3 phosphorylation [2]. sb505124 was shown to have no toxicity to renal epithelial a498 cells at concentrations up to 100 μm for 48 h. evidence showed that 100% drug will release within 12 h, and the gel showed no cytotoxicity to the cultured rabbit subconjunctival cells[2]. it was observed that alk4 downstream effectors including psmad2, ctgf, and α-sma was inhibited by sb505124 in cultured fibroblasts [3].in rabbit in glaucoma filtration surgery (gfs) model, the period of filtering blebs were reduced by tgfβ induced fibroblast. the filtering blebs in the gfs with sb505124 group were maintained for more than 10 days, and the period of bleb survival was significantly longer than that in controls, which suggested the significant inhibition of alk4 and 5 by sb505124 [2]. it was observed that alk4 downstream effectors ctgf and α-sma were suppressed by sb-505124 in vivo[3].

References

[1]. dacosta b s et al. sb-505124 is a selective inhibitor of transforming growth factor-beta type i receptors alk4, alk5, and alk7. mol pharmacol., 2004,65(3): 744-52.
[2]. sutariya v, et al. thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor sb-505124 for glaucoma filtration surgery. pharm dev technol., 2013, 18(4): 957-962.
[3]. sapitro j, et al. suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. mol vis., 2010, 16: 1880-1892.

SB-505124Supplier

Hangzhou Sage Chemical Co., Ltd.
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+86057186818502 13588463833
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info@sagechem.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
MedChemexpress LLC
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021-58955995
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ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185 18149758185
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sales-cpd@caerulumpharma.com
Shanghai Taifu Pharmaceutical Technology Co. LTD
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021-58111238 18930958102
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sales@taifupharm.com