2-APB (2-Aminoethyl Diphenylborinate)

Catalog No.S6657 Batch:S665701

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

23 mg/mL (102.18 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	1.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.)

Preparing Stock Solutions

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 4-Phenylbutyric acid (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 4-Phenylbutyric acid (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 11 publications

Matrix stiffness aggravates osteoarthritis progression through H3K27me3 demethylation induced by mitochondrial damage [ iScience, 2024, 27(8):110507]	PubMed: 39156637
Mild therapeutic hypothermic protection activates the PI3K/AKT signaling pathway to inhibit TRPM7 and suppress ferroptosis induced by myocardial ischemia‑reperfusion injury [ Mol Med Rep, 2024, 30(6)220]	PubMed: 39364741
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
Overexpression of Rhodopsin or Its Mutants Leads to Energy Metabolism Dysfunction in 661w Cells [ Invest Ophthalmol Vis Sci, 2022, 63(13):2]	PubMed: 36469028
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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