| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Antifibrotic agent 1 (compound 22) (0.001-10 μM, 48 hours) showed significant antifibrotic activity, inhibiting COL1A1 expression in A549 cells by 95.0% at a concentration of 1 μM, with an IC50 of 40.5 nM [1]. Antifibrotic agent 1 (1-200 μM) showed antifibrotic effects in A549, HEK293 and L02 cells, with low cytotoxicity (CC50 > 200 μM) [1]. Antifibrotic agent 1 (0.1-10 μM, 48 hours) dose-dependently reduced COL1A1 protein levels and inhibited epithelial-mesenchymal transition (EMT) and fibroblast-mesenchymal transition (FMT) processes associated with idiopathic pulmonary fibrosis (IPF) in TGF-β stimulated A549, HFL1 and HLFs cells [1]. Antifibrotic agent 1 (1–10 μM, 48 h) selectively inhibits the polarization of bone marrow-derived macrophages (BMDM) to the profibrotic M2 phenotype at a concentration of 10 μM [1]. Antifibrotic agent 1 (1–100 nM) selectively inhibits CSF-1R, PDGFR-α, and SFKs to alleviate IPF progression without affecting VEGFR, FGFR, and Abl to minimize off-target toxicity [1].
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| ln Vivo |
Antifibrotic drug 1 (compound 22) (60 mg/kg, orally, once daily for 14 days) has moderate oral bioavailability and good safety profile. No significant hepatotoxicity or nephrotoxicity was observed at doses up to 60 mg/kg in a bleomycin-induced mouse pulmonary fibrosis model [1]. Antifibrotic drug 1 (60 mg/kg, orally, once daily for 10 days) has excellent antifibrotic efficacy, significantly reducing pulmonary fibrosis in a bleomycin-induced mouse pulmonary fibrosis model, reducing the levels of inflammatory and pro-fibrotic M2-related cytokines, and improving lung function [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A549 cells, HFL1 cells, HLFs cells Tested Concentrations: 0.1, 0.5, 1, 10 μM Incubation Duration: 48 hours after TGF-β stimulation Experimental Results: In IPF-related EMT and FMT models and primary human lung fibroblast models, COL1A1 protein levels decreased in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Male C57BL/6 mice (8 weeks old) were administered bleomycin (BLM, 1.8 mg/kg) via intratracheal administration to induce pulmonary fibrosis [1].
Doses: 30 and 60 mg/kg Route of Administration: Oral administration (po), once daily for 14 days, followed by measurement of mouse body weight and lung tissue weight, and collection of lung tissue. Experimental Results: Significantly reduced mouse body weight loss, improved survival rate, enhanced lung function, and increased lung coefficient. At a dose of 60 mg/kg, Tgf-β mRNA expression was significantly downregulated in mouse lung tissue, and the mRNA and protein levels of Fn1 and Col1a1 were decreased, as was the hydroxyproline content. Significantly reduced TNF and Ccl2 mRNA levels, but increased IL-10 mRNA levels, thereby modulating the inflammatory response and further alleviating pulmonary fibrosis in mice. It strongly downregulated M2-related genes (Arg1, Mrc1) but did not affect the M1 marker CD86. It selectively inhibited the polarization of M2 macrophages in a mouse model, but had no significant effect on M1 polarization. At a dose of 60 mg/kg, it effectively alleviated pathological changes associated with pulmonary fibrosis and reduced collagen fibers, resulting in a 54.6% reduction in the pulmonary fibrosis area in a mouse model. |
| References |
| Molecular Formula |
C27H23CLN6O2
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|---|---|
| Molecular Weight |
498.96
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC(NC1=CC=C(C(Cl)=C1)NC(C2=CC=C(C(C#CC3=CC(C4=CN(N=C4)C)=CN=C3N)=C2)C)=O)=O
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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 | 2.0042 mL | 10.0208 mL | 20.0417 mL | |
| 5 mM | 0.4008 mL | 2.0042 mL | 4.0083 mL | |
| 10 mM | 0.2004 mL | 1.0021 mL | 2.0042 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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