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| Product Name: | BTP2 | | Synonyms: | BTP2;N-[4-[3,5-BIS(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]PHENYL]-4-METHYL-1,2,3-THIADIAZOLE-5-CARBOXAMIDE;4-methyl-4μ-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]-1,2,3-thiadiazole-5-carboxanilide;YM-58483;BTP 2, N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide;YM-5883;CRAC Channel Inhibitor, BTP2;YM-58483(BTP2) | | CAS: | 223499-30-7 | | MF: | C15H9F6N5OS | | MW: | 421.32 | | EINECS: | | Product Categories: | | Mol File: | 223499-30-7.mol |
| 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 |
| Uses | CRAC Channel Inhibitor BTP2 is a cell-permeable analog of BTP. A pyrazole derivative which inhibits activation-induced Ca2+ influx in rats. | | 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. |
| BTP2 Preparation Products And Raw materials |
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