EST64454

CAS No. 1950569-11-5

EST64454( —— )

Catalog No. M22978 CAS No. 1950569-11-5

EST64454 is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 174 In Stock
5MG 255 In Stock
10MG 407 In Stock
25MG 671 In Stock
50MG 945 In Stock
100MG 1251 In Stock
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Biological Information

  • Product Name
    EST64454
  • Note
    Research use only, not for human use.
  • Brief Description
    EST64454 is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.
  • Description
    EST64454 is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.
  • In Vitro
    ——
  • In Vivo
    EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively.EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% were 1178 ng/mL, <1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively. Animal Model:Male Wistar rats (250-300 g) Dosage:10 mg/kg Administration:P.o. (Pharmacokinetic Analysis) Result:The Cmax, t1/2, AUC0-∞, Vss and F% were 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively.
  • Synonyms
    ——
  • Pathway
    Autophagy
  • Target
    Sigma receptor
  • Recptor
    σ1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1950569-11-5
  • Formula Weight
    400.85
  • Molecular Formula
    C18H23ClF2N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?H2O : ≥ 100 mg/mL (249.47 mM))
  • SMILES
    CC(N1CCN(CCOCC2=NN(C3=CC=C(F)C(F)=C3)C=C2)CC1)=O.[H]Cl
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.José Luis Díaz, Mónica García, Torrens A , et al. EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management[J]. Journal of Medicinal Chemistry, 2020, 63(23):14979-14988.
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