203890-M

CRAC Channel Inhibitor, BTP2

The CRAC Channel Inhibitor, BTP2, also referenced under CAS 223499-30-7, controls the biological activity of CRAC Channel. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): CRAC Channel Inhibitor, BTP2, [N-{4-[3,5-bis(Trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methyl-1,2,3-thiadiazole-5-carboxamide], TPRC3 Channel Inhibitor II, Pyr2
• Empirical Formula (Hill Notation): C₁₅H₉F₆N₅OS
• CAS Number: 223499-30-7
• Molecular Weight: 421.32
• MDL number: MFCD00220976
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C15H9F6N5OS/c1-7-12(28-25-23-7)13(27)22-8-2-4-9(5-3-8)26-11(15(19,20)21)6-10(24-26)14(16,17)18/h2-6H,1H3,(H,22,27)
• InChI key: XPRZIORDEVHURQ-UHFFFAOYSA-N

Description

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 Ca^{2+ 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.}

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.

Biochem/physiol Actions

Primary Target
CRAC Channel

Target IC₅₀: 590 nM by Fura-2

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Schleifier, H., et al. 2012. Br J PharmacolIn Press
Yonetoku, Y., et al. 2006. Bioorg. Med. Chem.14, 5370.
Yonetoku, Y., et al. 2006. Bioorg. Med. Chem.14, 4750.
Zitt, C., et al. 2004. J. Biol. Chem.279, 12927.
Trevillyan, J.M., et al. 2001. J. Biol. Chem.276, 48118.
Djuric, S.W., et al. 2000. J. Med. Chem.43, 2975.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable