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HomeProduct name listBTP2

BTP2

Synonym(s):[N-{4-[3,5-bis(Trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methyl-1,2,3-thiadiazole-5-carboxamide], TPRC3 Channel Inhibitor II, Pyr2;4-methyl-4′-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]-1,2,3-thiadiazole-5-carboxanilide;CRAC Channel Inhibitor, BTP2 - CAS 223499-30-7 - Calbiochem

BTP2 Structural

What is BTP2?

The Uses of BTP2

CRAC Channel Inhibitor BTP2 is a cell-permeable analog of BTP. A pyrazole derivative which inhibits activation-induced Ca2+ influx in rats.

What are the applications of Application

CRAC Channel Inhibitor, BTP2 is a cell-permeable analog of BTP

General Description

A cell-permeable pyrazole that acts as a more potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 590 nM by Fura-2; peak current density pA/pF = -1.13 and -7.50, respectively, with or without 3 μM BTP2/Pyr2 by whole cell clamp) than the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) inTRPC3-expressing HEK293 cells (IC50 = 4.21 μM by Fura-2; pA/pF = -1.54 and -18.50, respectively, with or without 3 μM BTP2/Pyr2). A great complement to Pyr 3 (Cat. No. 648490), Pyr6, and Pyr10 in Ca2+ signaling studies.

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.

storage

Store at +4°C

Properties of BTP2

Melting point: 165-167 °C
Density  1.63±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: soluble10mg/mL, clear
pka 10.53±0.70(Predicted)
form  Solid
color  white to beige

Safety information for BTP2

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for BTP2

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