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.

• Synonyma: 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
• Empirický vzorec (Hillův zápis): C₁₅H₉F₆N₅OS
• Číslo CAS: 223499-30-7
• Molekulová hmotnost: 421.32
• UNSPSC Code: 12352200
• MDL number: MFCD00220976
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Quality Segment: 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
• SMILES string: FC(F)(F)c1[n](nc(c1)C(F)(F)F)c2ccc(cc2)NC(=O)c3[s]nnc3C
• 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

Popis

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.

Biochem/physiol Actions

Primary Target
CRAC Channel

Target IC₅₀: 590 nM by Fura-2

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• Co se děje?: WGK 3
• Bod vzplanutí (°F): Not applicable
• Bod vzplanutí (°C): Not applicable