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1204401-49-9

1204401-49-9 structure
1204401-49-9 structure
  • Name: WQ 1
  • Chemical Name: 2-(1-Benzyl-4-piperidinyl)-2,3-dihydro-4H-thiochromen-4-one
  • CAS Number: 1204401-49-9
  • Molecular Formula: C21H23NOS
  • Molecular Weight: 337.47800
  • Catalog: Signaling Pathways GPCR/G Protein Sigma Receptor
  • Create Date: 2018-12-16 12:42:43
  • Modify Date: 2024-01-16 19:52:06
  • σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1].

Name 2-(1-Benzyl-4-piperidinyl)-2,3-dihydro-4H-thiochromen-4-one
Description σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1].
Related Catalog
In Vitro σ1 Receptor antagonist-1 (compound 9) (10 μM; 48 hours) inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1]. Cell Cycle Analysis[1] Cell Line: MCF-7/ADR, MCF-7 cells Concentration: 10 μM Incubation Time: 48 hours Result: Increased the number of cells in G0/G1 (27.8%) and decreased those in S phase (46.7%), in a sigma 1-dependent manner. It selectively affects the high sigma 1 receptor expressing MCF-7/ADR but not the low sigma 1 receptor expressing MCF-7 cells.
In Vivo Pretreatment withσ1 Receptor antagonist-1 (1 mg/kg; s.c.) significantly increases the anti-nociceptive effect produces by morphine over the entire time course starting at 60 min[1]. Animal Model: Male CD-1 mice[1] Dosage: 1 mg/kg Administration: S.c. Result: Significantly increased the anti-nociceptive effect produced by morphine over the entire time course starting at 60 min.
References

[1]. Piergentili A, et al. Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. J Med Chem. 2010;53(3):1261-1269.

Molecular Formula C21H23NOS
Molecular Weight 337.47800
Exact Mass 337.15000
PSA 45.61000
LogP 4.58380
HS Code 2934999090

~74%

1204401-49-9 structure

1204401-49-9

Literature: Piergentili, Alessandro; Amantini, Consuelo; Del Bello, Fabio; Giannella, Mario; Mattioli, Laura; Palmery, Maura; Perfumi, Marina; Pigini, Maria; Santoni, Giorgio; Tucci, Paolo; Zotti, Margherita; Quaglia, Wilma Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1261 - 1269
Precursor  2

DownStream  0

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%