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Xestospongin C

IP3 receptor inhibitor
 
BML-CA409-0050 50 µg 519.00 USD
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Replaces Prod. #: ALX-350-382

Xestonspongin C is a structurally novel marine alkaloid isolated from the Okinawan sponge Xestospongia sp. It is a potent, cell-permeable inhibitor of IP3 receptor-mediated Ca2+ release (IC50 = 358 nM). However, since xestospongin C also inhibits voltage-dependent Ca2+ and K+ currents at concentrations similar to those which inhibit the IP3 receptor, it can only be regarded as a selective blocker of the IP3 receptor in permeabilized cells and not in cells with intact plasma membranes. Has vasodilatory properties.

Product Details

Formula:C28H50N2O2
 
MW:446.7
 
Source:Synthetic.
 
CAS:88903-69-9
 
Purity:≥90% (TLC)
 
Appearance:White to off-white powder.
 
Solubility:Soluble in DMSO or 100% ethanol at 2mM.
 
Shipping:Blue Ice
 
Long Term Storage:-20°C
 
Handling:Protect from light. Packaged under inert gas.
 
Regulatory Status:RUO - Research Use Only
 
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Product Literature References

Luminal H2O2 promotes ER Ca2+ dysregulation and toxicity of palmitate in insulin-secreting INS-1E cells: S. Sharifi, et al.; FASEB J. 37, e22685 (2023), Abstract;
Inhibitory mechanism of xestospongin-C on contraction and ion channels in the intestinal smooth muscle: H. Ozaki, et al.; Br. J. Pharmacol. 137, 1207 (2002), Abstract;
Xestospongin C empties the ER calcium store but does not inhibit InsP3-induced Ca2+ release in cultured dorsal root ganglia neurones: N. Solovyova, et al.; Cell Calcium 21, 49 (2002), Abstract;
Xestospongin C is a potent inhibitor of SERCA at a vertebrate synapse: A. Castonguay & R. Robitaille; Cell Calcium 32, 39 (2002), Abstract;
Ca2+ entry mediated by store depletion, S-nitrosylation, and TRP3 channels. Comparison of coupling and function: D.B. van Rossum, et al.; J. Biol. Chem. 275, 28562 (2000), Abstract;
In vivo signal transduction of nociceptive response by kyotorphin (tyrosine-arginine) through Galpha(i)- and inositol trisphosphate-mediated Ca(2+) influx: H. Ueda & M. Inoue; Mol. Pharmacol. 57, 108 (2000), Abstract;
Xestospongin C, a selective and membrane-permeable inhibitor of IP(3) receptor, attenuates the positive inotropic effect of alpha-adrenergic stimulation in guinea-pig papillary muscle: S. Miyamoto, et al.; Br. J. Pharmacol. 130, 650 (2000), Abstract;
Xestospongin C is an equally potent inhibitor of the inositol 1,4,5-trisphosphate receptor and the endoplasmic-reticulum Ca(2+) pumps: P. De Smet, et al.; Cell Calcium 26, 9 (1999), Abstract;
New developments in the molecular pharmacology of the myo-inositol 1,4,5-trisphosphate receptor: A. Wilcox, et al.; Trends Pharmacol. Sci. 19, 467 (1998), Abstract;
Xestospongins: potent membrane permeable blockers of the inositol 1,4,5-trisphosphate receptor: J. Gafni, et al.; Neuron 19, 723 (1997), Abstract;
Clinical and hematological studies on twelve cases of secondary aplastic anemia: M. Kobayashi, et al.; Nippon Ketsueki Gakkai Zasshi 47, 195 (1984), Abstract;
Structures of xestospongin A,B,C and D, novel vasodilativecompounds from marine sponge, Xestospongia exigua: M. Nakagawa, et al.; Tetrahedron Lett. 25, 3227 (1984),

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