| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
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| Targets |
ISX-3 targets the expression of PPARγ, a master regulator of cellular differentiation. PPARγ is a nuclear receptor that plays a pivotal role in promoting the differentiation of mesenchymal stem cells into adipocytes (fat cells) while inhibiting their differentiation into osteoblasts (bone-forming cells). By increasing PPARγ expression, ISX-3 may shift the balance of differentiation, promoting osteogenesis and suppressing adipogenesis, which could be beneficial in conditions like osteoporosis where bone formation is impaired and marrow adiposity is increased.
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| ln Vitro |
ALP induction is inhibited and lipid droplet accumulation is stimulated by ISX-3 (0-100,000 nM; 10 days) [1]. Western blot study of growing hBMSCs in the presence of MDI using ISX-3 (50 µM; 2 days) [1]
In vitro, ISX-3 demonstrates potent anti-adipogenic and pro-osteogenic activity. It increases the expression of PPARγ. In cell-based assays, it promotes the differentiation of precursor cells into osteoblasts, as evidenced by increased mineralization and expression of osteogenic markers, while inhibiting their differentiation into adipocytes. |
| ln Vivo |
In vivo, ISX-3 has the potential to treat osteopenia and osteoporosis. Its ability to promote bone formation and inhibit fat accumulation in the bone marrow could lead to increased bone mass and reduced fracture risk. Specific animal studies, including dosing and administration routes, are not detailed in the provided literature but are likely reported in other sources on this compound.
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| Enzyme Assay |
The activity of ISX-3 is typically assessed in cell-based assays using mesenchymal stem cells or pre-osteoblast cell lines. Cells are treated with the compound, and its effect on PPARγ expression is measured by qRT-PCR or Western blot. Its pro-osteogenic effect is assessed by measuring alkaline phosphatase activity, mineralization (alizarin red staining), and the expression of osteogenic markers like Runx2 and osteocalcin. Its anti-adipogenic effect is assessed by Oil Red O staining and the expression of adipogenic markers.
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| Cell Assay |
Western blot analysis
Tested Concentrations: 50µM Incubation Duration: 2 days Experimental Results: In MDI (0.5mM isobutylmethylxanthine, 1µM The expression levels of PPARγ are increased in the presence of dexamethasone and 1). μM insulin). The cellular activity of ISX-3 is evaluated in stem cell or precursor cell models of differentiation. Cells are treated with the compound during the differentiation process, and the resulting cell fate (osteoblast vs. adipocyte) is determined using the assays described above. |
| Animal Protocol |
In animal studies, ISX-3 would typically be administered to rodent models of osteoporosis, such as ovariectomized mice. The compound's effect on bone mineral density, bone volume, and bone turnover markers would be assessed using techniques like micro-CT, histomorphometry, and serum biomarker analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ISX-3 are not detailed in the provided literature. As a small molecule (MW 330.77), its absorption, distribution, metabolism, and excretion would need to be characterized for in vivo applications.
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| Toxicity/Toxicokinetics |
No specific toxicology data for ISX-3 is provided. As a research compound, its safety profile has not been established.
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| References |
[1]. Nawa K, et al. Discovering small molecules that inhibit adipogenesis and promote osteoblastogenesis: unique screening and Oncostatin M-like activity. Differentiation. 2013 Jul-Sep;86(1-2):65-74.
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| Additional Infomation |
ISX-3 (CAS: 912789-08-3) is a promising research tool for studying bone biology and developing therapies for osteoporosis. Its ability to modulate PPARγ expression to promote bone formation while inhibiting fat accumulation represents a novel approach to treating bone loss.
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| Molecular Formula |
C16H15CLN4O2
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|---|---|
| Exact Mass |
330.088
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| CAS # |
912789-08-3
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| PubChem CID |
22427445
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
398
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=CC(=C1)C1=CC(C(NCCCN2C=NC=C2)=O)=NO1
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| InChi Key |
DPAAHSSAGAOLBZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15ClN4O2/c17-13-4-1-3-12(9-13)15-10-14(20-23-15)16(22)19-5-2-7-21-8-6-18-11-21/h1,3-4,6,8-11H,2,5,7H2,(H,19,22)
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| Chemical Name |
5-(3-chlorophenyl)-N-(3-imidazol-1-ylpropyl)-1,2-oxazole-3-carboxamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~302.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.56 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 (7.56 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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