IBMX (Synonyms: Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine, NSC 165960, SC-2964) |
رقم الكتالوجGC11730
One-Click Copy Product Info
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يعد IBMX مثبطًا واسع النطاق لفوسفوديستراز (PDE) ، مع IC50s 6.5 و 26.3 و 31.7 ميكرومتر لـ PDE3 و PDE4 و PDE5 ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 28822-58-4
Sample solution is provided at 25 µL, 10mM.
IBMX is a non-specific inhibitor of phosphodiesterase (PDE) inhibitor that inhibits PDE3, PDE4 and PDE5 with IC50 values of 6.5, 26.3 and 31.7 µm, except PDE8A, PDE8B and PDE9[1,7].
In cardiac H9c2 cells,IBMX reduced loss of δψm caused by H(2)O(2), indicating that inhibition of PDEs can prevent the mPTP opening. However, IBMX could not inhibit the pore opening in cells transfected with the constitutively active GSK-3β (GSK-3β-S9A) mutant, suggesting a critical role of GSK-3β in the action of IBMX. IBMX also reduced reperfusion injury in a GSK-3β dependent manner[5]. Increasing cAMP-signaling with Forskolin or IBMX significantly facilitated neuronal functional maturation. A continuous application of IBMX to the differentiation medium substantially increased the functional expression of voltage-gated Na(+) and K(+) channels, as well as neuronal firing frequency[6].
Chronic exposure to cold caused pulmonary arterial hypertension and increased phosphodiesterase-1C (PDE-1C) expression in pulmonary arteries (PAs) in rats. After 8-week exposure to cold, Treatment with 8-IBMX significantly attenuated the cold-induced increase in right ventricular pressure. Cold exposure also caused right-ventricular hypertrophy, whereas 8-IBMX reversed cold-induced right ventricular hypertrophy. 8-IBMX abolished cold-induced upregulation of PDE-1C in PAs[4]. In hyperglycemic rat, all test compounds decreased blood glucose and the effect of milrinone was potentiated by glybenclamide. Milrinone or IBMX did not change plasma insulin levels, but it was augmented by combination of milrinone and glybenclamide. In both species, liver glycogen storage was decreased by IBMX, mc5, mc6 or MCPIP, increased by mc2 and was not changed in the presence of mc1[3]. ANG II increased ROMK channel activity in CCDs isolated from high-K (HK)-fed but not normal K (NK)-fed rats. Pretreatment of CCDs with IBMX, a broad-spectrum PDE inhibitor, or cilostamide, a PDE3 inhibitor, abolished the stimulatory effect of ANG II on ROMK channels[2].
References:
[1]: Wu BN, Lin RJ, et,al. KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. doi: 10.1038/sj.bjp.0705791. Epub 2004 Jul 5. PMID: 15237094; PMCID: PMC1575170.
[2]: Wei Y, Liao Y,et,al. Angiotensin II type 2 receptor regulates ROMK-like K? channel activity in the renal cortical collecting duct during high dietary K? adaptation. Am J Physiol Renal Physiol. 2014 Oct 1;307(7):F833-43. doi: 10.1152/ajprenal.00141.2014. Epub 2014 Aug 6. PMID: 25100281; PMCID: PMC4187043.
[3]: Hosseini A, Shafiee-Nick R, et,al. Differential metabolic effects of novel cilostamide analogs, methyl carbostiryl derivatives, on mouse and hyperglycemic rat. Iran J Basic Med Sci. 2012 Jul;15(4):916-25. PMID: 23493150; PMCID: PMC3586914.
[4]: Crosswhite P, Sun Z. Inhibition of phosphodiesterase-1 attenuates cold-induced pulmonary hypertension. Hypertension. 2013 Mar;61(3):585-92. doi: 10.1161/HYPERTENSIONAHA.111.00676. Epub 2013 Jan 14. PMID: 23319544; PMCID: PMC4050371.
[5]: Chanoit G, Zhou J,et,al. Inhibition of phosphodiesterases leads to prevention of the mitochondrial permeability transition pore opening and reperfusion injury in cardiac H9c2 cells. Cardiovasc Drugs Ther. 2011 Aug;25(4):299-306. doi: 10.1007/s10557-011-6310-z. PMID: 21643720.
[6]: Lepski G, Jannes CE, et,al. cAMP promotes the differentiation of neural progenitor cells in vitro via modulation of voltage-gated calcium channels. Front Cell Neurosci. 2013 Sep 19;7:155. doi: 10.3389/fncel.2013.00155. PMID: 24065885; PMCID: PMC3777016.
[7]: Soderling SH, Bayuga SJ, et,al. Identification and characterization of a novel family of cyclic nucleotide phosphodiesterases. J Biol Chem. 1998 Jun 19;273(25):15553-8. doi: 10.1074/jbc.273.25.15553. PMID: 9624145.
| Kinase experiment [1]: | |
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Preparation Method |
Purified protein containing PDE3, 4 or 5 enzyme was resuspended in 50 mM Tris HCl containing 5 mM MgCl2 (pH 7.5). Subsequently, the enzyme (11.5 mg ml 1, 10 μl) was incubated with Tris HCl (80 μl) and 10 μM cyclic GMP or cyclic AMP substrate (final concentration 1 μM containing 0.1 μCi [3H]-cyclic GMP or [3H]-cyclic AMP) was added. After 20 min at 37 °C, the samples were heated to 100 °C for 2 min. Ophiophagus hannah snake venom (10 mg ml 1, 10 μl) was then added and incubated at 37 °C for 10 min to convert the 5 -GMP and 5 -AMP to the uncharged nucleosides, guanosine and adenosine, respectively. An ion-exchange resin (200 μl) was added to bind all unconverted cyclic GMP or cyclic AMP. IBMX as inhibitor, used to inhibit PDE detection IC50. |
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Reaction Conditions |
IBMX 10 mM in DMSO |
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Applications |
IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor that inhibits PDE3,PDE4 and PDE5 with IC50 values of 6.5,26.3 and 31.7 μm, respectively. |
| Cell experiment [2]: | |
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Cell lines |
Cortical collecting duct (CCD) |
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Preparation Method |
Cells were grown in 24-well plates with 105 cells per well at confluence, monolayers were washed with phosphate buffer solution (PBS) and incubated with KMUP-1 (0.1-100μM) in the presence of 100uM IBMX for 20 min by adding 10% trichloroacetic acid (TCA) to stop the incubation. |
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Reaction Conditions |
100μM IBMX for 20 minutes |
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Applications |
IBMX(100 μM) activated ROMK channels and prevented further channel activation by ANG II or cGMP. |
| Animal experiment [3]: | |
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Animal models |
Six groups of male Sprague–Dawley rats were used (150-180 g) |
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Preparation Method |
After 8 weeks of exposure to cold, 3 groups in each temperature condition received continuous intravenous infusion of 8-isobutyl-methylxanthine (8-IBMX) (PDE-1 inhibitor, 8.5 mg/kg per day),apocynin and vehicle. |
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Dosage form |
8.5 mg/kg/day for 1 week |
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Applications |
Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantly reduces medial layer thickness and increases lumen diameter of small PAs in cold-exposed rats. |
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References: [1]. Wu BN, Lin RJ,et,al. KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. doi: 10.1038/sj.bjp.0705791. Epub 2004 Jul 5. PMID: 15237094; PMCID: PMC1575170. [2]. Wei Y, Liao Y,et,al. Angiotensin II type 2 receptor regulates ROMK-like K? channel activity in the renal cortical collecting duct during high dietary K? adaptation. Am J Physiol Renal Physiol. 2014 Oct 1;307(7):F833-43. doi: 10.1152/ajprenal.00141.2014. Epub 2014 Aug 6. PMID: 25100281; PMCID: PMC4187043. [3]. Crosswhite P, Sun Z. Inhibition of phosphodiesterase-1 attenuates cold-induced pulmonary hypertension. Hypertension. 2013 Mar;61(3):585-92. doi: 10.1161/HYPERTENSIONAHA.111.00676. Epub 2013 Jan 14. PMID: 23319544; PMCID: PMC4050371. |
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| Cas No. | 28822-58-4 | SDF | |
| المرادفات | Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine, NSC 165960, SC-2964 | ||
| Chemical Name | 3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione | ||
| Canonical SMILES | O=C(N(C)C1=O)N(C2=C1NC=N2)CC(C)C | ||
| Formula | C10H14N4O2 | M.Wt | 222.24 |
| الذوبان | ≥ 9.45mg/mL in DMSO; Insoluble in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4996 mL | 22.4982 mL | 44.9964 mL |
| 5 mM | 899.9 μL | 4.4996 mL | 8.9993 mL |
| 10 mM | 450 μL | 2.2498 mL | 4.4996 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)