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MedChemExpressModel Xestospongin C -88903-69-9

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Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells[1][2][3].
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Xestospongin C

MCE China:Xestospongin C

Brand:MedChemExpress (MCE)

Cat. No.HY-103312

CAS:88903-69-9

Synonyms:(-)-Xestospongin C

Purity:99.0%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells.

In Vitro:Xestospongin C (XeC; 10 μM; 1 h before Aβ) pretreatment before Aβ1-42 (20 μM; 24 hours) application displays a significant decrease in the early apoptotic rate (9.87%) compared to the Aβ alone treated group (18.38%)[1]. Xestospongin C (10 μM; 1 h before Aβ) and Aβ1-42 (20 μM; 100 s) has significant main effects on the peak value and average values of Ca2+ changes, as well as a significant interaction in primary cultured hippocampal neurons[1].

In Vivo:Xestospongin C (3 μM; intracerebroventrical injection by a pump for four weeks) ameliorates the disinhibition-like behavior and long term spatial memory deficits of 8-month-old male APP/PS1 mice of Alzheimer's disease[1].

IC50 & Target:IP3R

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References:

[1]. Wang ZJ, et al. Xestospongin C, a Reversible IP3 Receptor Antagonist, Alleviates the Cognitive and Pathological Impairments in APP/PS1 Mice of Alzheimer's Disease. J Alzheimers Dis. 2019;72(4):1217-1231.  [Content Brief]

[2]. Gafni J, Munsch JA, Lam TH, Catlin MC, Costa LG, Molinski TF, Pessah IN. Xestospongins: potent membrane permeable blockers of the inositol 1,4,5-trisphosphate receptor. Neuron. 1997 Sep;19(3):723-33. doi: 10.1016/s0896-6273(00)80384-0. PMID: 9331361.  [Content Brief]

[3]. Castonguay A, et al. Xestospongin C is a potent inhibitor of SERCA at a vertebrate synapse. Cell Calcium. 2002;32(1):39-47.  [Content Brief]

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