2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel TRP Channel CRAC Channel
  4. 2-Aminoethyl diphenylborinate

2-Aminoethyl diphenylborinate  (Synonyms: 2-APB)

Cat. No.: HY-W009724 Purity: 98.86%
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2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue.

For research use only. We do not sell to patients.

CAS No. : 524-95-8

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Customer Review

Based on 71 publication(s) in Google Scholar

2-Aminoethyl diphenylborinate Related Antibodies

Top Publications Citing Use of Products

71 Publications Citing Use of MCE 2-Aminoethyl diphenylborinate

Cell Imaging/Staining
Flow Cytometry
Cell Proliferation/Viability Assay
WB

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Oct 5;13(10):e012182.  [Abstract]

    Confocal microscopy analysis of cellular calcium overloading in BMDMs after osimertinib stimulation with or without ML-SI3 (5µM) or 2-APB (10µM; 30 min) pretreatment.

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Nov 10;23(1):1254.  [Abstract]

    Effect of different calcium ion channel blockers oncell death. HCMEC were pretreated with Dizocilpine (10 µM), Nifedipine (10 µM) and 2-APB (100 µM) for 1 h and then treated with Hcy and CuCl2 underH/R condition for 24 h. Cell death was analyzed by LDH release assay

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Nov 10;23(1):1254.  [Abstract]

    HCMECs were pretreated with 2-APB (100 µM) for 1 h and then treated with Hcy and CuCl2 under H/R condition for 24 h. Effect of 2-APB on total intracellular and mitochondrial calcium.

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Sep 19;22(1):578.  [Abstract]

    The effect of 2-APB (0, 25, 50, 100 μM; 2+24 h) on the expression of polarization marker proteins iNOS and Arg-1 in RAW264.7 cells after LPS/IL-4 treatment.

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2021 Nov;8(21):e2101936.  [Abstract]

    HCT116 cells were pretreated with 2-APB (10 × 10−6 M) for 1 h, followed by SR140333 treatment for 24 h. cell viability was measured by trypan blue exclusion assay.

    2-Aminoethyl diphenylborinate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2021 Nov;8(21):e2101936.  [Abstract]

    Western blotting in HCT116 cells treated with SR140333 (38 × 10−6 m) for 24 h after pretreatment with BAPTA-AM (10 ×10−6 M) or 2-APB (10 × 10−6 M) for 1 h.

    View All Calcium Channel Isoform Specific Products:

    View All Isoforms
    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue[1][2][3][4][5].

    IC50 & Target

    Inositol triphosphate receptor (IP3R)
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    1 μM
    Compound: 2-APB
    Inhibition of human TRPM2 expressed in HEK293 cells
    Inhibition of human TRPM2 expressed in HEK293 cells
    		[PMID: 24304219]
    Jurkat IC50
    15 μM
    Compound: 2-APB
    Inhibition of thapsigargin-induced SOCE channel in fura-2 loaded human Jarkart T cells in presence of 2 mM calcium
    Inhibition of thapsigargin-induced SOCE channel in fura-2 loaded human Jarkart T cells in presence of 2 mM calcium
    		[PMID: 20097561]
    In Vitro

    2-Aminoethyl diphenylborinate (2-APB) (10-100 μM, 2 min) evokes external acid-dependent increases of [Ca2+] and dopamine release in PC12 cells through the activation of Orai 3[3].
    2-Aminoethyl diphenylborinate (100 μM, 9 h) provides protective effects against ischemia-reperfusion (I/R)-induced damage in Hep G2 cells[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    2-Aminoethyl diphenylborinate Related Antibodies
    In Vivo

    2-Aminoethyl diphenylborinate (0.5 or 2 mg/kg, i.p., administered for 24 hours) exhibited an inhibitory effect on vasospasm in Sprague-Dawley rats[2].
    2-Aminoethyl diphenylborinate (2 or 4 mg/kg, i.p., single administration for 10 min) reduces the oxidative stress and apoptosis caused by testicular ischemia-reperfusion injury in rats[4].
    2-Aminoethyl diphenylborinate (2 mg/kg, i.v. (via portal vein), 10 min before ischemia) is effective in preventing hepatic Ischemia-reperfusion (I/R) damage when administered via the portal vein before ischemiain an in mice model of liver Ischemia-reperfusion (I/R) injury[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Ischemia-reperfusion-induced testicular injury Sprague Dawley rats model (weighting 250-300 g)[4]
    Dosage: 2 or 4 mg/kg
    Administration: Intravenous injection (i.v.) (via portal vein), 10 min before ischemia
    Result: Decreased serum alanine aminotransferase (AST), aspartate aminotransferase (ALT), and lactate dehydrogenase (LDH) following ischemia-reperfusion (I/R).
    Animal Model: Subarachnoid hemorrhage (SAH) Sprague-Dawley rats model (induced by injecting blood from the right femoral artery into the cisterna magna, rats weighting 250-300 g)[2]
    Dosage: 0.5 or 2 mg/kg
    Administration: Intraperitoneal (i.p.)
    Result: Increased the basilar artery wall thickness and reduced the basilar artery lumen diameter, inducing significant vascular changes (sampled 24 hours after administration).
    Alleviated cell apoptosis at 24 hours after subarachnoid hemorrhage (sampled 24 hours after administration).
    Animal Model: Male Sprague Dawley rats model of hepatic Ischemia-reperfusion (I/R) [5]
    Dosage: 2 mg/kg
    Administration: Intraperitoneal (i.p.)
    Result: Significantly increased total antioxidant capacity and glutathione levels, and decreased malondialdehyde content, DNA fragmentation, and the number of TUNEL (Terminal deoxynucleotidyl transferase dUTP nick end labeling) positive cells (measured 10 minutes after administration).
    Molecular Weight

    225.09

    Formula

    C14H16BNO
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NCCOB(C1=CC=CC=C1)C2=CC=CC=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (1110.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1.61 mg/mL (7.15 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.4427 mL 22.2133 mL 44.4267 mL
    5 mM 0.8885 mL 4.4427 mL 8.8853 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (9.24 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (9.24 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *The compound is unstable in solutions, freshly prepared is recommended.

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 4.4427 mL 22.2133 mL 44.4267 mL 111.0667 mL
    5 mM 0.8885 mL 4.4427 mL 8.8853 mL 22.2133 mL
    DMSO 10 mM 0.4443 mL 2.2213 mL 4.4427 mL 11.1067 mL
    15 mM 0.2962 mL 1.4809 mL 2.9618 mL 7.4044 mL
    20 mM 0.2221 mL 1.1107 mL 2.2213 mL 5.5533 mL
    25 mM 0.1777 mL 0.8885 mL 1.7771 mL 4.4427 mL
    30 mM 0.1481 mL 0.7404 mL 1.4809 mL 3.7022 mL
    40 mM 0.1111 mL 0.5553 mL 1.1107 mL 2.7767 mL
    50 mM 0.0889 mL 0.4443 mL 0.8885 mL 2.2213 mL
    60 mM 0.0740 mL 0.3702 mL 0.7404 mL 1.8511 mL
    80 mM 0.0555 mL 0.2777 mL 0.5553 mL 1.3883 mL
    100 mM 0.0444 mL 0.2221 mL 0.4443 mL 1.1107 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    2-Aminoethyl diphenylborinate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    2-Aminoethyl diphenylborinate524-95-82-APBCalcium ChannelTRP ChannelCRAC ChannelCa2+ channelsCa channelsTransient receptor potential channelsCalcium release-activated channelsCa2+ release-activated Ca2+ channelsSprague-Dawley ratsAnti-inflammatory activity VasospasmInhibitorinhibitorinhibit

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