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2-Aminoethyl diphenylborinate

Name: 2-Aminoethyl diphenylborinate
Brand: TargetMol
SKU: T4693
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: 2-APB, 2-Aminoethoxydiphenyl borate) Copy Product Info

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Synonyms: 2-APB, 2-Aminoethoxydiphenyl borate

Catalog No. T4693 Copy Product Info

Purity: 99.92%

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2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R and TRP channels. 2-Aminoethyl diphenylborinate also inhibits store-operated Ca2+ (SOC) channels and activates certain TRP channels (V1, V2, and V3). 2-Aminoethyl diphenylborinate also inhibits vasospasm. 2-Aminoethyl diphenylborinate can be used in research on calcium biology, cell signaling, oncology, and neurobiology.

Cas No. 524-95-8

Pack Size	Price	USA Stock	Global Stock
10 mg	$30	In Stock	In Stock
25 mg	$65	In Stock	In Stock
50 mg	$92	In Stock	In Stock
100 mg	$129	In Stock	In Stock
500 mg	$319	-	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.92%

Appearance:solid

Color:White

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Product Introduction

2-Aminoethyl diphenylborinate AI Summary

2-Aminoethyl diphenylborinate exhibits broad bioactivity across various biological pathways and targets. It demonstrates significant growth inhibition against Mycobacterium tuberculosis H37Rv with a MIC of 71,000 nM in Bactec 6A media and 285,000 nM in Bactec 12B media. It also inhibits the thapsigargin-induced SOCE channel in fura-2 loaded human Jarkart T cells with an IC50 of 15,000 nM. Notably, it functions as an agonist at TRPV1, TRPV2, and TRPV3 with activity at 10 µM. In additional assays, it shows moderate to high potency in inhibiting multiple targets, including Menin-MLL Interaction, Thyroid Hormone Receptor, Jumonji Domain Containing 2E, Tyrosyl-DNA Phosphodiesterase, Cruzain, Aldehyde Dehydrogenase 1, Bacillus subtilis Sfp phosphopantetheinyl transferase, and others. 2-Aminoethyl diphenylborinate also exhibits antiviral activity against SARS-CoV-2 and Foot and Mouth Disease Virus. It demonstrates inhibitory activity against human TRPM2 in HEK293 cells with an IC50 of 1,000 nM and effectively reduces ADPR-induced intracellular calcium flux. Furthermore, it acts as an inhibitor of rabbit skeletal muscle microsomes FITC-labelled SERCA1a and porcine cerebellar microsomes FITC-labelled SERCA2b, both with an IC50 of 70,000 nM. Lastly, it shows potential as an HDAC6 inhibitor with significant activity in enzymatic assays..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R and TRP channels. 2-Aminoethyl diphenylborinate also inhibits store-operated Ca2+ (SOC) channels and activates certain TRP channels (V1, V2, and V3). 2-Aminoethyl diphenylborinate also inhibits vasospasm. 2-Aminoethyl diphenylborinate can be used in research on calcium biology, cell signaling, oncology, and neurobiology.
Targets & IC50	IP3:42 μM
In vitro	Methods: RAW264.7 mouse macrophages were pretreated with 2-Aminoethyl diphenylborinate (0, 25, 50, 100 μM) for 2 hours, then co-incubated with LPS (1000 ng/mL) or IL-4 (20 ng/mL) for 24 hours. Western blot analysis detected M1/M2 markers iNOS (M1), Arg-1 (M2), and immunofluorescence analysis for iNOS⁺ and Arg-1⁺ cells. Results: 2-Aminoethyl diphenylborinate dose-dependently reduced iNOS protein expression while increasing Arg-1 and CD206 levels. Immunofluorescence confirmed that 2-Aminoethyl diphenylborinate decreased iNOS⁺ cells and increased Arg-1⁺ cells. [1] Methods: Neonatal rat atrial myocytes (NRAMs) expressing the cytoplasmic cAMP FRET sensor EPAC-SH187 were preincubated with 2-Aminoethyl diphenylborinate (2.5 μM) for 20 min. Following PE (3 μM) stimulation, cAMP levels were monitored in real-time for approximately 20 min. Results: 2-Aminoethyl diphenylborinate pretreatment significantly suppressed PE-induced FRET elevation, reducing the peak to 5.89 ± 5.66%. [2]
In vivo	Methods: DBA/1J mice, collagen-induced arthritis (CIA) model. Starting from day 28 post-immunization, intra-articular injections of 2-Aminoethyl diphenylborinate@DGP-MM (5 μL/joint, 100 μM solution) were administered every 4 days until day 49, totaling approximately 3 weeks of treatment. Results: The 2-Aminoethyl diphenylborinate@DGP-MM treatment group demonstrated the most significant effects in reducing arthritis scores, alleviating paw swelling, and improving joint pathology scores. [1]
Synonyms	2-APB, 2-Aminoethoxydiphenyl borate

Chemical Properties

Molecular Weight	225.09
Formula	C₁₄H₁₆BNO
Cas No.	524-95-8
Smiles	NCCOB(c1ccccc1)c1ccccc1
Relative Density.	1.04 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 255 mg/mL (1132.88 mM), Sonication is recommended.

Ethanol: 10 mM, Heating is recommended.

In Vivo Formulation

5% DMSO+95% Saline: 1.13 mg/mL (5.02 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.4427 mL	22.2133 mL	44.4267 mL	222.1334 mL
5 mM	0.8885 mL	4.4427 mL	8.8853 mL	44.4267 mL
10 mM	0.4443 mL	2.2213 mL	4.4427 mL	22.2133 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.2221 mL	1.1107 mL	2.2213 mL	11.1067 mL
50 mM	0.0889 mL	0.4443 mL	0.8885 mL	4.4427 mL
100 mM	0.0444 mL	0.2221 mL	0.4443 mL	2.2213 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Related Tags: 2-Aminoethyl diphenylborinate chemical structure | 2-Aminoethyl diphenylborinate in vivo | 2-Aminoethyl diphenylborinate in vitro | 2-Aminoethyl diphenylborinate formula | 2-Aminoethyl diphenylborinate molecular weight