CALP1 TFA

• CAT Number: I045739
• Molecular Formula: C42H76F3N9O12
• Molecular Weight: 956.10
• Purity: ≥95%
• Synonyms: (2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]hexanoic acid;2,2,2-trifluoroacetic acid
• InChI: InChI=1S/C40H75N9O10.C2HF3O2/c1-13-23(10)31(48-33(51)24(11)43-35(53)28(42)20(4)5)38(56)49-32(25(12)50)39(57)47-30(22(8)9)37(55)45-27(18-19(2)3)34(52)46-29(21(6)7)36(54)44-26(40(58)59)16-14-15-17-41;3-2(4,5)1(6)7/h19-32,50H,13-18,41-42H2,1-12H3,(H,43,53)(H,44,54)(H,45,55)(H,46,52)(H,47,57)(H,48,51)(H,49,56)(H,58,59);(H,6,7)/t23-,24-,25+,26-,27-,28-,29-,30-,31-,32-;/m0./s1
• InChIKey: NEQKOMDEJDLJON-KIFCWDIHSA-N
• SMILES: CCC(C)C(C(=O)NC(C(C)O)C(=O)NC(C(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)O)NC(=O)C(C)NC(=O)C(C(C)C)N.C(=O)(C(F)(F)F)O

CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity[1][2][3][4].

Reference

[1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.
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[2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.
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[3]. M K Manion, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.
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[4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.
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