| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
ISX-1 does not have a defined classical drug target like a receptor or enzyme. It is a phenotypic modulator that affects cell differentiation. It promotes the differentiation of mesenchymal stem cells towards the osteoblast lineage while inhibiting their differentiation into adipocytes.
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|---|---|
| ln Vitro |
In addition to inducing ALP with an EC50 value of 1.2 μM, ISX-1 can construct lipid droplets with an IC50 value of 1.9 μM [1]. PPARγ and FABP4 gene mRNA induction during lipid secretion in hBMSCs is inhibited by ISX-1 (0, 1.3, 6.5, and 33 μM; 3 days) [1]. TCF/LEF-mediated gene transcription is facilitated by ISX-1 (0, 1.3, 6.5, and 33 μM)[1].
In vitro, ISX-1 dose-dependently inhibits the accumulation of intracellular lipid droplets. It stimulates alkaline phosphatase (ALP) activity, a marker of osteoblast differentiation. This confirms its anti-adipogenic and pro-osteogenic activities in cell-based models. |
| ln Vivo |
In vivo efficacy of ISX-1 is implied by its use in research for osteoporosis and osteopenia. While specific in vivo data is not detailed in the provided sources, its pro-osteogenic and anti-adipogenic activities suggest it could be effective in animal models of bone loss.
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| Enzyme Assay |
ISX-1 is not typically evaluated in direct enzyme/receptor binding assays. Its activity is assessed in cell-based functional assays that measure its effects on cell differentiation. These assays focus on its ability to modulate the differentiation of stem or progenitor cells.
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| Cell Assay |
RT-PCR[1]
Cell Types: human bone marrow mesenchymal stem cells (hBMSCs) Tested Concentrations: 0, 1.3, 6.5 and 33 μM Incubation Duration: 3 days Experimental Results: Inhibits mRNA induction. PPARγ and FABP4 genes have no effect on C/EBPα expression during adipogenic differentiation of hBMSCs. Western Blot Analysis[1] Cell Types: HEK 293 Cell Tested Concentrations: 6.5 and 33 μM Incubation Duration: 6.5 and 33 μM Experimental Results: The amount of activated β-catenin and total β-catenin increased. In vitro experiments involve treating mesenchymal stem cells or pre-adipocyte cell lines with ISX-1. Adipogenesis is assessed by measuring lipid accumulation (e.g., Oil Red O staining), while osteogenesis is assessed by measuring ALP activity or mineralization. |
| Animal Protocol |
In vivo animal models for ISX-1 would likely involve models of osteoporosis, such as ovariectomized (OVX) mice or rats. Animals would be treated with the compound, and bone mineral density and microarchitecture would be assessed. The compound's effect on bone formation and fat accumulation would be evaluated.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for ISX-1 is not provided in the sources. As a research compound, its properties are being investigated. Its molecular formula and weight are available in chemical databases. Its suitability for in vivo studies is implied by its research applications.
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| Toxicity/Toxicokinetics |
Toxicological data for ISX-1 is not detailed in the provided sources. As a research compound, it is not intended for human use. Its safety profile would need to be established through preclinical studies if it were to be developed further.
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| References |
[1]. Nawa, Katsuhiko 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-1 is a research tool for studying the balance between adipogenesis and osteogenesis. Its ability to promote bone formation while inhibiting fat formation makes it a potential candidate for treating osteoporosis and other bone diseases. It represents a novel approach to bone anabolic therapy.
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| Molecular Formula |
C14H14N4O2S
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|---|---|
| Molecular Weight |
302.351561069489
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| Exact Mass |
302.083
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| CAS # |
909207-35-8
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| PubChem CID |
3235911
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| Appearance |
White to light yellow solid powder
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| LogP |
1.4
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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 |
6
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| Heavy Atom Count |
21
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| Complexity |
358
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C(C2SC=CC=2)=CC(C(NCCCN2C=NC=C2)=O)=N1
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| InChi Key |
LRGVDHZAEYAHLG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14N4O2S/c19-14(16-4-2-6-18-7-5-15-10-18)11-9-12(20-17-11)13-3-1-8-21-13/h1,3,5,7-10H,2,4,6H2,(H,16,19)
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| Chemical Name |
N-(3-imidazol-1-ylpropyl)-5-thiophen-2-yl-1,2-oxazole-3-carboxamide
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| Synonyms |
ISX1; ISX 1; ISX-1
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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: ~50 mg/mL (~165.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (8.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.27 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3074 mL | 16.5371 mL | 33.0743 mL | |
| 5 mM | 0.6615 mL | 3.3074 mL | 6.6149 mL | |
| 10 mM | 0.3307 mL | 1.6537 mL | 3.3074 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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