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YM 58483

YM 58483

Catalog No.

B7542

A store-operated Ca²⁺ entry (SOCE) blocker

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Size	Price	Stock	Qty
10mg	$154.00	In stock
50mg	$561.00	In stock

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Background
Product Citation
Chemical Properties
Protocol
Quality Control

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.

Product Citation

1. Ziping Cheng, Yangjie Liu, et al. "Lansoprazole-Induced Osteoporosis via IP3R and SOCE Mediated Calcium Signaling Pathway." Mol Med. 2022 Feb 19;28(1):21. PMID: 35183103

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	421.32
Cas No.	223499-30-7
Formula	C₁₅H₉F₆N₅OS
Solubility	insoluble in H2O; ≥50 mg/mL in EtOH; ≥90 mg/mL in DMSO
Chemical Name	N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide
SDF	Download SDF
Canonical SMILES	FC(F)(C1=CC(C(F)(F)F)=NN1C(C=C2)=CC=C2NC(C3=C(C)N=NS3)=O)F
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

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

Quality Control & MSDS

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Purity = 99.79%

Chemical structure

YM 58483

mRNA synthesis

Tyramide Signal Amplification (TSA)

Phos Binding Reagent Acrylamide

Cell Counting Kit-8 (CCK-8)

Inhibitor Cocktails

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Quality Control & MSDS

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