874374-25-1

874374-25-1 structure
874374-25-1 structure
  • Name: Ned 19
  • Chemical Name: 1-(3-{[4-(2-Fluorophenyl)-1-piperazinyl]methyl}-4-methoxyphenyl)- 2,3,4,9-tetrahydro-1H-β-carboline-3-carboxylic acid
  • CAS Number: 874374-25-1
  • Molecular Formula: C30H31FN4O3
  • Molecular Weight: 514.59100
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
  • Create Date: 2016-01-31 08:49:47
  • Modify Date: 2024-01-02 10:15:55
  • Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM[1]. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice[2].

Name 1-(3-{[4-(2-Fluorophenyl)-1-piperazinyl]methyl}-4-methoxyphenyl)- 2,3,4,9-tetrahydro-1H-β-carboline-3-carboxylic acid
Description Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM[1]. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice[2].
Related Catalog
Target

Ca2+

In Vitro Ned 19 (25-100 μM; 24-72 hours) reduces cell proliferation[2]. Ned 19 (25-100 μM; 24-72 hours) reduces markedly the cell number[2]. Ned 19 (25-100 μM; 24-72 hours) reduces the S phase percentage and increases of the G0/G1 phase percentage evaluated by cell cycle analysis[2]. Ned 19 (25-100 μM; 24-72 hours) induces cell apoptosis a time-dependent manner[2]. Ned 19 (25-100 μM; 24-72 hours) reduces expression of N-cadherin and increases expression of E-cadherin, affecting the cell migratory behavior[2]. Cell Proliferation Assay[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced cell proliferation. Cell Viability Assay[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced markedly the cell number. Cell Cycle Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced the S phase percentage and increased of the G0/G1 phase percentage. Apoptosis Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Induced cell apoptosis a time-dependent manner. Western Blot Analysis[2] Cell Line: B16 cells Concentration: 25, 50, 100 μM Incubation Time: 24, 48, 72 hours Result: Reduced expression of N-cadherin and increased expression of E-cadherin.
In Vivo Ned 19 (i.p.; 5 mg/Kg/every second day; 4 week) impaires severely tumor growth[2]. Animal Model: Adult male C57BL/6 mice[2] Dosage: 5 mg/Kg Administration: I.p.; every second day; 4 week Result: Impaired severely tumor growth.
References

[1]. Rosen D, et al. Analogues of the nicotinic acid adenine dinucleotide phosphate (NAADP) antagonistNed-19 indicate two binding sites on the NAADP receptor. J Biol Chem. 2009 Dec 11;284(50):34930-4.

[2]. Annarita Favia, et al. NAADP-Dependent Ca2+ Signaling Controls Melanoma Progression, Metastatic Dissemination and Neoangiogenesis. Sci Rep. 2016; 6: 18925.

Molecular Formula C30H31FN4O3
Molecular Weight 514.59100
Exact Mass 514.23800
PSA 80.83000
LogP 4.65780