| 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
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| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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