| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In a quantitative and time-dependent manner, the treatment of THP-1 macrophage-derived foam cells with Ibrolipim (0.5-10 μM) elevates the translational levels of ABCA1 and ABCG1 expression [1]. A dose- and time-dependent manner is shown in the rise of ABCA1 and ABCG1 expression at transcript levels following treatment with ibrolipim (0.5-10 μM; 0-24 hours; THP-1 macrophage-derived foam cells) [1]. Ibrolipim 5 and 50 μMol/L markedly enhanced the efflux of cholesterol from foam cells generated from THP-1 macrophages to either apoA-I or HDL. Ibrolipim therapy also resulted in an upregulation of LXRα. LXRα small interfering RNA eliminated the Ibrolipim-induced promotion effect entirely. [1]
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| ln Vivo |
Treatment with Ibrolipim (NO-1886; 100 mg/kg; vascular wall; daily; for 8 weeks; Sprague-Dawley deposition in females) prevented weight gain following ovariectomy and decreased visceral fat buildup. In the liver, soleus muscle, and mesenteric fat, ibrolipim decreases the quotient and increases the expression of translocase messenger RNA (mRNA). Additionally, ibrolipim raises the expression of uncoupling protein 3 (UCP3) mRNA in the heart, soleus muscle, and mesenteric fat, but not in brown adipose tissue. It also raises the expression of graft-binding protein mRNA in the liver and soleus muscle [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-1 macrophage-derived foam cells Tested Concentrations: 0.5 μM, 5 μM, 10 μM Incubation Duration: 0 hrs (hours), 6 hrs (hours), 12 hrs (hours), 24 hrs (hours) Experimental Results: ABCA1 and ABCG1 translation levels increased in a dose-dependent and time-dependent manner. RT-PCR[1] Cell Types: THP-1 macrophage-derived foam cells Tested Concentrations: 0.5 μM, 5 μM, 10 μM Incubation Duration: 0 hrs (hours), 6 hrs (hours), 12 hrs (hours), 24 hrs (hours) Experimental Results: Increased expression of ABCA1 and ABCG1 Transcription levels were dose- and time-dependent. |
| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) Rat (10 weeks old; 200-260 g) Experimental Ovariectomy Treatment [2]
Doses: 100 mg/kg Route of Administration: Oral; daily; continued for 8 weeks Experimental Results: Visceral fat accumulation Reduce and suppress weight gain due to oophorectomy. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Ibrolipim has known human metabolites that include [4-[(4-Bromo-2-cyanophenyl)carbamoyl]phenyl]methyl-ethoxyphosphinic acid. |
| References |
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| Additional Infomation |
Ibrolipim is a lipoprotein lipase (LPL) activator with antihyperlipidemic activity. Activation of LDL by ibrolipim lowers plasma triglycerides, with a concomitant elevation of high-density lipoprotein cholesterol.
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| Molecular Formula |
C19H20BRN2O4P
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|---|---|
| Molecular Weight |
451.2568
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| Exact Mass |
450.034
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| CAS # |
133208-93-2
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| PubChem CID |
131601
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| Appearance |
White to yellow solid powder
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| Density |
1.44g/cm3
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| Boiling Point |
512.5ºC at 760 mmHg
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| Flash Point |
263.7ºC
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| Vapour Pressure |
1.29E-10mmHg at 25°C
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| Index of Refraction |
1.59
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| LogP |
5.412
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
576
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KPRTURMJVWXURQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20BrN2O4P/c1-3-25-27(24,26-4-2)13-14-5-7-15(8-6-14)19(23)22-18-10-9-17(20)11-16(18)12-21/h5-11H,3-4,13H2,1-2H3,(H,22,23)
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| Chemical Name |
N-(4-bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide
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| Synonyms |
OPF 009; NO-1886; Ibrolipim
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~110.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2160 mL | 11.0801 mL | 22.1602 mL | |
| 5 mM | 0.4432 mL | 2.2160 mL | 4.4320 mL | |
| 10 mM | 0.2216 mL | 1.1080 mL | 2.2160 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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