223499-30-7

Usage

Uses

Used in CRAC Channel Inhibition:
BTP2 is used as a CRAC channel inhibitor for its ability to block activation-induced Ca2+ influx in rats. This makes it a valuable tool in studying the role of CRAC channels in various cellular processes.
Used in Ca2+ Signaling Studies:
BTP2 is used as a research tool in Ca2+ signaling studies to investigate the function and regulation of Stim1 and Orai1-coupled CRAC channels, as well as TRPC3-mediated ROCE. Its potency and selectivity make it a valuable complement to other pyrazole derivatives like Pyr 3, Pyr6, and Pyr10.
Used in Drug Discovery and Development:
BTP2 can be used in the development of drugs targeting CRAC channels and related pathways, potentially leading to treatments for various diseases and conditions associated with Ca2+ signaling dysregulation.
Used in Cellular Physiology Research:
BTP2 is used in cellular physiology research to study the mechanisms of store-operated Ca2+ entry and receptor-operated Ca2+ entry, providing insights into the complex interplay of Ca2+ signaling pathways in cells.

Biological Activity

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.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.

Biochem/physiol Actions

YM-58483 is a selective Ca++ release-activated Ca++ (CRAC) [a.k.a. store-operated Ca++ (SOC) channels] that mediate Ca++ influx in T cells and other inflammatory cells. CRAC channel inhibitors have potential clinical applications in autoimmune disease, transplant rejection, allergic airway inflammation and bronchial asthma. YM-58483 is also promoted as a tool for CRAC studies; may be used as a gold standard.