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YM 58483

Catalog No.
B7542
A store-operated Ca2+ entry (SOCE) blocker
Grouped product items
SizePriceStock Qty
10mg
$154.00
In stock
50mg
$561.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

YM 58483, also known as BTP2, is a SOCE blocker. SOCE has been found in macrophages, basophils, dendritic cells, and mast cells as well as T cells. The SOCE-related channels include the Ca2+ release-activated Ca2+ (CRAC) channel which is a highly Ca2+-selective channel, and the non-selective, Ca2+-permeable transient receptor potential (TRP) channels, which regulate the activation of non-excitable cells such as lymphocytes. YM 58483 has been reported to inhibit cytokine production and proliferation in T cells, and may serve as a potential medicinal candidate for treatment of bronchial asthma. 

References:

1. Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792.

2. Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt421.32
Cas No.223499-30-7
FormulaC15H9F6N5OS
Solubilityinsoluble in H2O; ≥50 mg/mL in EtOH; ≥90 mg/mL in DMSO
Chemical NameN-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
SDFDownload SDF
Canonical SMILESFC(F)(C1=CC(C(F)(F)F)=NN1C(C=C2)=CC=C2NC(C3=C(C)N=NS3)=O)F
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while.

Protocol

Cell experiment:[2]

Cell lines

Jurkat cells

Reaction Conditions

0.0003 ~ 1 μM YM 58483

Applications

YM 58483 dose-dependently inhibited PHA-induced IL-2 production in Jurkat cells, with an IC50 value of 17 ± 3.2 nM. Moreover, YM 58483 potently inhibited NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells.

Animal experiment:[1]

Animal models

Mouse graft-versus-host disease (GVHD) model

Dosage form

1 ~ 30 mg/kg

Once daily by oral route (p.o.) for 10 days

Applications

YM 58483 (1 ~ 30 mg/kg, p.o.) and cyclosporine A (1 ~ 30 mg/kg, p.o.) inhibited donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduced the number of donor T cells, especially donor CD8+ T cells, in the spleen.

Note

The technical data provided above is for reference only.

References:

1. Ohga K, Takezawa R, Arakida Y, et al. Characterization of YM-58483/BTP2, a novel store-operated Ca2+ entry blocker, on T cell-mediated immune responses in vivo. International Immunopharmacology, 2008, 8(13-14): 1787-1792.

2. Ishikawa J, Ohga K, Yoshino T, et al. A pyrazole derivative, YM-58483, potently inhibits store-operated sustained Ca2+ influx and IL-2 production in T lymphocytes. Journal of Immunology, 2003, 170(9): 4441-4449.

Quality Control

Chemical structure

YM 58483