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Atrasentan

CAS No. 173937-91-2

Atrasentan( ABT-627 | (+)-A 127722 | A-147627 )

Catalog No. M23784 CAS No. 173937-91-2

Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 111 In Stock
5MG 92 In Stock
10MG 132 In Stock
25MG 264 In Stock
50MG 368 In Stock
100MG 600 In Stock
200MG 825 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock
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Biological Information

  • Product Name
    Atrasentan
  • Note
    Research use only, not for human use.
  • Brief Description
    Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).
  • Description
    Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).
  • In Vitro
    Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM).
  • In Vivo
    Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model.
  • Synonyms
    ABT-627 | (+)-A 127722 | A-147627
  • Pathway
    GPCR/G Protein
  • Target
    Endothelin Receptor
  • Recptor
    ET-A
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    173937-91-2
  • Formula Weight
    510.62
  • Molecular Formula
    C29H38N2O6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (184.27 mM)
  • SMILES
    CCCCN(CCCC)C(CN(C[C@@H]([C@H]1C(O)=O)c(cc2)cc3c2OCO3)[C@H]1c(cc1)ccc1OC)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Yuyama H, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol. 2004 Sep 13;498(1-3):171-7.
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