1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. IBMX

IBMX  (Synonyms: 3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine)

Cat. No.: HY-12318 Purity: 99.99%
SDS COA Handling Instructions

IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.

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

IBMX Chemical Structure

IBMX Chemical Structure

CAS No. : 28822-58-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of IBMX:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE IBMX

WB

    IBMX purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331.  [Abstract]

    The combination of Fsk and IBMX (Fsk-IBMX) inhibits the expression of cAMP related protein. The results of Western blot in glioma stem cells (GSCs).

    IBMX purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Jan;120(1):321-331.  [Abstract]

    U0126 enhances the negative effect of Fsk-IBMX on the development of glioma stem cells (GSCs).

    View All Phosphodiesterase (PDE) Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.

    IC50 & Target

    PDE3

     

    PDE4

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    466 μM
    Compound: IBMX
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    In Vitro

    At 100 μM, KMUP-1 (a xanthine derivative) and IBMX are the most effective at inducing tracheal relaxation; the magnitude of the relaxation responses induced by KMUP-1 and IBMX are not significantly different[1]. IBMX (100 μM) activates renal outer medullary K+ (ROMK) channels (n=6, P<0.05) and prevents further channel activation by ANG II (n=6, P=NS) or cGMP. Of note is that pretreatment of cortical collecting duct (CCDs) isolated from high-K+ (HK)-fed rats with IBMX (100 μM) for 20 min leads to a significant increase in tubular cAMP content to 1.43±0.35 pg/mm tubule length (n=14) compare with that measured in vehicle-treated controls (0.61±0.13 pg/mm tubule length, n=12, P<0.05)[2].

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

    In Vivo

    IBMX, a non-selective PDE inhibitor significantly decreases the liver glycogen storage (mg/g, IBMX 22±1.5 P<0.001). In comparison with the control group, IBMX and mc5 significantly increase plasma glucose (blood glucose, mg/dl, control=141±3, IBMX=210±17 P<0.001 and mc5=191±13 P<0.01) while other test compounds (mc1, mc6, MCPIP and Win 47203) do not produce significant effect (control=141±3, mc1 160±7, mc6 175±9, MCPIP 179±8 and Win 47203 116±2 P>0.05) also mc2 does not change plasma glucose (control=141±3 and mc2=145±5). IBMX has the highest efficacy on increasing plasma glucose[3]. Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure (23.5±1.8 and 24.2±0.6 mmHg, respectively) although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantly reduces medial layer thickness (19.0±0.9, and 16.9±0.8 μm, respectively) and increases lumen diameter (62.7±4.2, and 59.5±4.3 μm, respectively) of small PAs in cold-exposed rats[4].

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

    Molecular Weight

    222.24

    Formula

    C10H14N4O2

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N1C)N(CC(C)C)C2=C(N=CN2)C1=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (562.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : ≥ 7.14 mg/mL (32.13 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.4996 mL 22.4982 mL 44.9964 mL
    5 mM 0.8999 mL 4.4996 mL 8.9993 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    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: ≥ 1.67 mg/mL (7.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 1.67 mg/mL (7.51 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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 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

    Purity: 99.99%

    References
    Cell Assay
    [2]

    Cells are grown in 24-well plates 105 cells per well. At confluence, monolayer cells are washed with phosphate buffer solution (PBS) and then incubated with KMUP-1 (0.1-100 μM) in the presence of 100 μM IBMX for 20 min. Incubation is terminated by the addition of 10% trichloroacetic acid (TCA). Cell suspensions are sonicated and then centrifuged at 2500× g for 15 min at 4°C. To remove TCA, the supernatants are extracted three times with 5 volumes of water-saturated diethyl ether. Then, the supernatants are lyophilized and the cyclic GMP or AMP of each sample is determined by using commercially available radioimmunoassay kits[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    Male mice (25-35 g) are used. For the experiment, the test compound (IBMX, MCPIP, mc1, mc2, mc5 or mc6) or solvent (control) is injected subcutaneously to mice at 1 mg/kg dosage twice a day (8:00 a.m. and 8:00 p.m.) for 7 days.
    Rats[4]
    Six groups of male Sprague-Dawley rats are used (150-180g, 6 rats/group). Three groups of rats are exposed to a climate-controlled walk-in chamber maintained at moderate cold (5.0±1°C). The remaining groups are kept in an identical chamber maintained at room temperature (23.5±1°C, warm) and served as controls. After eight weeks of exposure to cold, 3 groups in each temperature condition received continuous IV infusion of IBMX (PDE-1 inhibitor, 8.5 mg/kg/day), Apocynin (NADPH oxidase inhibitor, 25 mg/kg/day) and vehicle (DMSO, 50%), respectively. The doses of drugs have been validated for effective inhibition of PDE-1 and NADPH oxidase activity, respectively. Body weight is measured weekly. After one week of drug infusion, the animals’ right ventricular systolic blood pressure (RVBP) is measured under anesthesia. The RVP is a reliable indicator of pulmonary arterial blood pressure (PAP) and has been used by numerous investigators for evaluating PH.

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

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 4.4996 mL 22.4982 mL 44.9964 mL 112.4910 mL
    5 mM 0.8999 mL 4.4996 mL 8.9993 mL 22.4982 mL
    10 mM 0.4500 mL 2.2498 mL 4.4996 mL 11.2491 mL
    15 mM 0.3000 mL 1.4999 mL 2.9998 mL 7.4994 mL
    20 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
    25 mM 0.1800 mL 0.8999 mL 1.7999 mL 4.4996 mL
    30 mM 0.1500 mL 0.7499 mL 1.4999 mL 3.7497 mL
    DMSO 40 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
    50 mM 0.0900 mL 0.4500 mL 0.8999 mL 2.2498 mL
    60 mM 0.0750 mL 0.3750 mL 0.7499 mL 1.8748 mL
    80 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
    100 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1249 mL
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    • 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.

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