2-APB (2-Aminoethyl Diphenylborinate)

Catalog No.S6657 Batch:S665702

Technical Data

Formula	C₁₄H₁₆BNO
Molecular Weight	225.09	CAS No.	524-95-8
Solubility (25°C)*	In vitro	DMSO	45 mg/mL (199.92 mM)
		Ethanol	45 mg/mL (199.92 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

2-APB (2-Aminoethyl Diphenylborinate) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.

Targets

IP3 receptor ^[1]

SOC channel ^[2]

TRP channel ^[2]

In vitro

2-APB, an inositol 1, 4, 5-trisphosphate receptor (IP₃R) inhibitor, obviously attenuates the intracellular Ca²⁺ release and cardiomyocyte apoptosis induced by oxygen and glucose deprivation (OGD) stimulation and EndoA2 knockdown.^[3]

In vivo

2-APB increases the basilar artery (BA) wall thickness and reduced the BA lumen diameter, inducing significant vascular changes, also alleviates cell apoptosis at 24 hours after SAH.^[4]

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines neonatal rat cardiomyocytes Concentrations 2 h Incubation Time -- Method Neonatal Sprague-Dawley rats (1 to 3 days old) are exposed to hypothermia until they became unresponsive and are then euthanized by cervical dislocation. Primary culture of NRCMs is performed. The cells are seeded at a density of 5 x 10⁶ cells/ml in Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum and 0.1 mM 5-bromodeoxyuridine. After 24 h, NRCMs are subjected to various treatments as described below. To assess the effects of EndoA2 on cardiac injury, the cells are transfected with EndoA2 siRNA or Ad-EndoA2. After transfection for 36 h, the cells are stimulated with oxygen and glucose deprivation (OGD) for another 12 h. Incubation of sodium phenylbutyrate (4-PBA), Cyclosporin A (CsA), 1,2-bis(o-aminophenoxy)ethane-N,N,N ,N -tetraacetic acid (BAPTA) or 2-Aminoethoxydiphenylborate (2-APB) is 2 h before OGD stimulation.Cardiomyocytes are cultured in serum-free, glucose and sodium pyruvate-free DMEM at 37 ℃ in an anoxia chamber saturated with 94% N₂/5% CO₂/ 1% O₂.
Animal Study:^{^[4]}	Animal Models Rats of subarachnoid hemorrhage (SAH) model Dosages 0.5, 2 mg/kg Administration i.p.

Cell Assay:^{^[3]}

Cell lines
neonatal rat cardiomyocytes
Concentrations
2 h
Incubation Time
--
Method
Neonatal Sprague-Dawley rats (1 to 3 days old) are exposed to hypothermia until they became unresponsive and are then euthanized by cervical dislocation. Primary culture of NRCMs is performed. The cells are seeded at a density of 5 x 10⁶ cells/ml in Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum and 0.1 mM 5-bromodeoxyuridine. After 24 h, NRCMs are subjected to various treatments as described below. To assess the effects of EndoA2 on cardiac injury, the cells are transfected with EndoA2 siRNA or Ad-EndoA2. After transfection for 36 h, the cells are stimulated with oxygen and glucose deprivation (OGD) for another 12 h. Incubation of sodium phenylbutyrate (4-PBA), Cyclosporin A (CsA), 1,2-bis(o-aminophenoxy)ethane-N,N,N ,N -tetraacetic acid (BAPTA) or 2-Aminoethoxydiphenylborate (2-APB) is 2 h before OGD stimulation.Cardiomyocytes are cultured in serum-free, glucose and sodium pyruvate-free DMEM at 37 ℃ in an anoxia chamber saturated with 94% N₂/5% CO₂/ 1% O₂.

Animal Study:^{^[4]}

Animal Models
Rats of subarachnoid hemorrhage (SAH) model
Dosages
0.5, 2 mg/kg
Administration
i.p.

References

[4] Boyacı MG, et al. World Neurosurg. 2019 Jul;127:e376-e388.

+ Expand

Selleck's 2-APB (2-Aminoethyl Diphenylborinate) has been cited by 8 publications

Porcine reproductive and respiratory syndrome virus infection triggers autophagy via ER stress-induced calcium signaling to facilitate virus replication [ PLoS Pathog, 2023, 19(3):e1011295]	PubMed: 36972295
Only one carbon difference determines the pro-apoptotic activity of α-tocopheryl esters [ FEBS J, 2022, 10.1111/febs.16623]	PubMed: 36083714
Endophilin A2-mediated alleviation of endoplasmic reticulum stress-induced cardiac injury involves the suppression of ERO1α/IP3R signaling pathway [ Int J Biol Sci, 2021, 17(13):3672-3688]	PubMed: 34512174
Endophilin A2-mediated alleviation of endoplasmic reticulum stress-induced cardiac injury involves the suppression of ERO1α/IP3R signaling pathway [ Int J Biol Sci, 2021, 17(13):3672-3688]	PubMed: 34512174
Evodiamine induces ROS-Dependent cytotoxicity in human gastric cancer cells via TRPV1/Ca2+ pathway [ Chem Biol Interact, 2021, 351:109756]	PubMed: 34808100
STIM1 Regulates Endothelial Calcium Overload and Cytokine Upregulation During Sepsis [ J Surg Res, 2021, 263:236-244]	PubMed: 33713955
Calcium channel blocker amlodipine besylate therapy is associated with reduced case fatality rate of COVID-19 patients with hypertension [ Cell Discov, 2020, 6(1):96]	PubMed: 33349633
CaSR participates in the regulation of vascular tension in the mesentery of hypertensive rats via the PLC‑IP3/AC‑V/cAMP/RAS pathway [ Mol Med Rep, 2019, 20(5):4433-4448]	PubMed: 31485595

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