| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
XRF-1021 (3-100 μM, 48 h) inhibited the proliferation of TGF-β1-stimulated NRK-49F cells with an IC50 value of 4.87 μM, indicating that it may regulate the HIPK2-mediated signaling pathway [1]. XRF-1021 (100 μM, 24 h) can directly bind to HIPK2 and exhibits high binding stability (RMSD approximately 0.1 Å, RMSF < 0.1 Å) [1]. XRF-1021 (2.5-80 μM, 24 h) had no significant effect on the proliferation or viability of HK-2 cells at concentrations of 2.5, 5, and 10 μM [1]. XRF-1021 (2.5-10 μM, 24 h) can inhibit HIPK2 and its downstream signaling pathways, thereby alleviating fibrosis in HK-2 cells [1]. XRF-1021 (2.5-10 μM, 24 h) can reduce the expression of HIPK2, FN and α-SMA proteins in NRK-49F cells [1].
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| ln Vivo |
XRF-1021 (25-75 mg/kg, vascular wall) inhibits the expression of fibrosis markers by suppressing HIPK2 and its downstream buffers, such as TGF-β, NF-κB, p53, Wnt/β-catenin and Notch staining, thereby attenuating the progression of renal fibrosis in the Sprague-Dawley (SD) report UUO model [1]. XRF-1021 (25-100 mg/kg, vascular wall) attenuates renal tubular damage, reduces interstitial fibrosis and improves renal function in the C57BL/6J renal tubular adenine diet model by inhibiting HIPK2 and its downstream multiple pro-fibrotic signal redundancy, including TGF-β, NF-κB, p53, Wnt/β-catenin and Notch buffer [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: TGF-β1-stimulated HK-2 cells Tested Concentrations: 2.5, 5, 10 μM Incubation Duration: 24 h Experimental Results: Reduced the expression levels of these fibrotic markers, including FN, α-SMA, and HIPK2 protein expression in HK-2 cells dose-dependently. Exhibited the most pronounced inhibitory effect at 10 μmol/L. Western Blot Analysis[1] Cell Types: TGF-β1-stimulated HK-2 cells Tested Concentrations: 0, 10 μM Incubation Duration: 24 h Experimental Results: Significantly attenuated the phosphorylation levels of both proteins, indicating effective suppression of the TGF-β and NF-κB pathways. Effectively reversed these TGF-β1-induced increases, including Wnt/β-catenin pathway target genes (PAI-1, Axin2, and MMP7) and Notch pathway target genes (Hes1, Hey1, and Hey2). |
| Animal Protocol |
Animal/Disease Models: Sprague-Dawley (SD) rats[1]
Doses: 25, 50 and 75 mg/kg Route of Administration: oral administration (p.o.) Experimental Results: Partially ameliorated these pathological changes in a dose-dependent manner, with the 75 mg/kg dose showing greater efficacy. Relieved renal injury and renal fibrosis and diminished the expression levels of related renal fibrosis indicators. Suppressed the protein expression of fibrotic markers (FN, Collagen I, α-SMA, Vimentin) and HIPK2. Inhibited HIPK2-regulated p53 pathway, TGF-β/Smad3, NF-κB, Wnt/β-catenin and Notch pathways. Animal/Disease Models: Male C57BL/6J mice (seven weeks)[1] Doses: 25, 50 and 100 mg/kg Route of Administration: oral administration (p.o.) Experimental Results: Mitigated renal lesions and interstitial fibrosis in a dose-dependent manner, with the 100 mg/kg dose showing the most pronounced effect. Reduced serum creatinine, blood urea nitrogen, and uric acid levels dose-dependently. Downregulated the expression of HIPK2, collagen I, α-SMA, and vimentin in the kidneys of adenine-fed mice. Reduced phosphorylation levels of Smad3, NF-κB and p53. |
| References |
| Molecular Formula |
C21H21FN8
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|---|---|
| Molecular Weight |
404.44
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| CAS # |
2968523-32-0
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| Appearance |
Typically exists as solids at room temperature
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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 | 2.4726 mL | 12.3628 mL | 24.7255 mL | |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 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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