Drug intelligence / Profile preview

BTP-2

Development stage
Preclinical
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

BTP-2 (also known as YM-58483) is a potent and selective small-molecule inhibitor of store-operated calcium entry (SOCE) and calcium release-activated calcium (CRAC) channels. It acts by blocking the influx of extracellular calcium mediated by the Orai-STIM complex, which is triggered following the depletion of intracellular calcium stores in the endoplasmic reticulum. BTP-2 is widely utilized as a pharmacological research tool to investigate the role of calcium signaling in immune cell activation, cytokine production (such as IL-2 and IL-4), and smooth muscle contraction. Preclinical studies have explored its potential in treating a variety of conditions, including asthma, acute lung and liver injuries, inflammatory pigmentary disorders, and certain cancers, where it often works by suppressing NFAT-mediated gene transcription and reducing inflammatory responses.

Other names
N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide3,5-bis(trifluoromethyl)pyrazole derivative 2
02

Targets

ORAI1 (Calcium release–activated calcium channel protein 1)ORAI2 (Orai calcium release-activated calcium modulator 2)RYR1 (Ryanodine receptor 1)ORAI3 (Calcium release-activated calcium channel protein 3)STIM1 (Stromal interaction molecule 1)

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