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xestospongin C
- Development stage
- Unknown
- Modality
- Small Molecules
- Administration
- In Vitro (primarily Cell-based/research Use)
01
Overview
Xestospongin C is a marine-derived macrocyclic bis-1-oxaquinolizidine natural product, first identified from *Xestospongia* sponges. It acts as a **potent, membrane-permeable antagonist of the inositol-1,4,5-trisphosphate receptor (IP3 receptor)**, thereby inhibiting IP3-mediated Ca2+ release from intracellular stores such as the endoplasmic and sarcoplasmic reticulum. Xestospongin C has been shown to block the IP3 receptor with nanomolar potency and is ~30-fold selective over the ryanodine receptor. It also inhibits the sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA) pumps at similar concentrations, thus it is not strictly selective for IP3 receptors. Xestospongin C has been primarily used as a **research tool** for investigating intracellular calcium signaling but is not approved for clinical use in humans or animals[1][2][3][5][7].
- Other names
- xestospongin CXeCAraguspongine E
02
Targets
CaV (Voltage-gated calcium channel protein complex)ATP2A (Sarcoplasmic reticulum Ca2+-ATPase)IP3R (Inositol Trisphosphate Receptor)Kir (Inward-rectifier potassium channels)
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