| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Fatty acid-binding protein 4 (FABP4/aP2).
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|---|---|
| ln Vitro |
THP-1 macrophages treated with BMS-309403 produced much less MCP-1 in a time- and dose-dependent manner[1].
BMS-309403 binds to the internal fatty acid-binding pocket of FABP4 and competitively inhibits endogenous fatty acid binding. It exhibits Ki values of <2 nM for FABP4, 250 nM for FABP3 (heart isoform), and 350 nM for FABP5, demonstrating >100-fold selectivity for FABP4. It also stimulates glucose uptake in myotubes via AMPK activation and decreases ER stress-associated inflammation. |
| ln Vivo |
While endothelium-independent relaxations were unaffected, BMS-309403 sodium (15 mg/kg; daily for 6 weeks) improved endothelial function, phosphorylated and total eNOS, and plasma triglyceride levels[3].
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| Enzyme Assay |
The FABP4 inhibitor screening assay uses a fluorescence polarization (FP)-based method. Recombinant human FABP4 protein is incubated with BMS-309403 sodium dilutions and a fluorescent fatty acid probe (e.g., 1-aminopyrene-3,6,8-trisulfonate). The displacement of the probe results in decreased fluorescence polarization. Ki values are calculated by fitting the competition binding data to a standard inhibition curve.
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| Cell Assay |
To assess cellular activity, FABP4-expressing adipocytes or macrophages are treated with BMS-309403 sodium (typically 1-10 uM). Endogenous fatty acid uptake is measured using fluorescent fatty acid analogs (e.g., BODIPY-labeled palmitate). The inhibition of lipolysis or inflammatory cytokine production (TNF-alpha, IL-6) is also measured by ELISA. Cell viability is confirmed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Animal/Disease Models: C57BL/6J mice (ApoE−/− mice)[3]
Doses: 15 mg/kg Route of Administration: Chronic treatment ; daily for 6 weeks Experimental Results: Dramatically increased the phosphorylated eNOS (Ser1177) and total eNOS but not the phosphorylated to total eNOS ratio in aortae of 18 weeks old ApoE−/− mice. In vivo studies are conducted in mouse models of diabetes, atherosclerosis, or acute lung injury. The compound is administered orally (e.g., 40 mg/kg daily). Endpoints include blood glucose levels, plasma lipid profiles, and tissue inflammation markers. In a CLP-induced ALI model, treatment improved survival and prevented lung inflammation and FABP4 upregulation. |
| ADME/Pharmacokinetics |
Detailed PK data are not fully published, but the compound is orally active, indicating it has adequate oral bioavailability. As a small molecule (MW ~474.55 for free acid), it likely distributes to adipose tissue and liver, where FABP4 is highly expressed. Its metabolism and excretion pathways require further characterization.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available. In animal studies (e.g., up to 6 weeks in mice), no significant body weight differences or overt adverse effects were reported. Standard preclinical studies would be required for development, including safety pharmacology (hERG, CNS, respiratory) and repeat-dose toxicity in two species.
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| References |
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| Additional Infomation |
BMS-309403 sodium is a research chemical, not an approved drug. It is the most widely used tool compound for studying FABP4 biology. It has shown therapeutic potential in preclinical models of type 2 diabetes, atherosclerosis, asthma, and cancer metastasis. The compound was originally developed by Bristol-Myers Squibb, and the sodium salt form is used to improve aqueous solubility.
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| Molecular Formula |
C31H27N2NAO3
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|---|---|
| Molecular Weight |
498.5474588871
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| Exact Mass |
496.176
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| CAS # |
2802523-05-1
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| Related CAS # |
BMS-309403;300657-03-8
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| PubChem CID |
155882742
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
696
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1N(C2C=CC=CC=2C2C=CC=C(OCC(=O)O)C=2)N=C(C2C=CC=CC=2)C=1C1C=CC=CC=1)C.[NaH]
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| InChi Key |
NZLJLBNAOJOVBZ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C31H26N2O3.Na/c1-2-27-30(22-12-5-3-6-13-22)31(23-14-7-4-8-15-23)32-33(27)28-19-10-9-18-26(28)24-16-11-17-25(20-24)36-21-29(34)35;/h3-20H,2,21H2,1H3,(H,34,35);/q;+1/p-1
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| Chemical Name |
sodium;2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O: 100 mg/mL (201.40 mM)
DMSO: 50 mg/mL (100.70 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 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 25.0 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. Solubility in Formulation 2: 2.5 mg/mL (5.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.0058 mL | 10.0291 mL | 20.0582 mL | |
| 5 mM | 0.4012 mL | 2.0058 mL | 4.0116 mL | |
| 10 mM | 0.2006 mL | 1.0029 mL | 2.0058 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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