White solid. HYGROSCOPIC. One of the most potent known agonist of type 1 inositol 1,4,5-trisphosphate receptor (InsP3R; EC50 = 10.9 nM). Exhibits about 50- to 100-fold greater affinity for IP3R than IP3. Stimulates Ca2+ release from Ins(1,4,5)P3-sensitive Ca2+ stores in microsomal preparations, permeabilized cells, and lipid vesicles containing purified InsP3R (EC50 = 14.7 nM for Ca2+ release from permeabilized hepatocytes). Does not bind to Ins(1,3,4,5)P4 binding sites and is resistant to enzymatic degradation. Purity: ≥90% by HPLC. Ref.: Correa, V., et al. 2001. Mol. Pharmacol. 59, 1206. Marchant, J.S., and Taylor, C.W. 1998. Biochemistry 37, 11524. DeLisle, S., et al. 1997. J. Biol. Chem. 272, 9956. Hartzell, H.C., et al. 1997. Mol. Pharmacol. 51, 683. Marchant, J.S., et al. 1997. Biochemistry 36, 12780. Hirota, J., et al. 1995. FEBS Lett. 368, 248. Takahashi, M., et al. 1994. J. Biol. Chem. 269, 369. |
