| ln Vitro |
BI-113823 (10⁻⁷-10⁻⁶ M; 12 h) inhibited TNF-α-induced migration of human peripheral blood mononuclear cells and human peripheral blood neutrophils in a dose-dependent manner [2]. BI-113823 (10⁻⁷-10⁻⁶ M) reduced LPS-induced TNF-α production in human peripheral blood mononuclear cells in a dose-dependent manner [2]. BI-113823 (10-100 nM) inhibited LPS-induced activation of human peripheral blood mononuclear cells and human peripheral blood neutrophils and reduced CD11/CD18 expression levels [2]. BI-113823 (10⁻⁷-10⁻⁶ M) reduced LPS-induced MPO activity in human peripheral blood neutrophils in a dose-dependent manner [2]. BI-113823 (1 μM; 24 h) inhibited TGF-β-induced expression of α-SMA in LX2 human hepatic stellate cells [2]. BI-113823 (0–2 μM; 24 h) reduced the expression of TGF-β-stimulated profibrotic protein and B1R and inhibited Akt phosphorylation in LX2 human hepatic stellate cell lines [2]. BI-113823 (0.1–1 μM; 0–48 h) dose-dependently inhibited TGF-β-induced contraction of LX2 human hepatic stellate cells in collagen gel [2]. BI-113823 (0.1–1 μM; 12 h) dose-dependently inhibited the migration of LX2 human hepatic stellate cell lines stimulated with 1% FBS [2]. BI-113823 (0.1–2 μM) inhibited DBK-induced scratch healing migration in human hepatic stellate cell line LX2 in a dose-dependent manner [2]. BI-113823 (0.001–1 μM) inhibited DBK-stimulated proliferation of human hepatic stellate cell line LX2 in a dose-dependent manner without affecting basal proliferation or inducing apoptosis [2]. BI-113823 (1 μM) inhibited the G1 phase to S phase cell cycle transition in DBK-stimulated human hepatic stellate cell line LX2 [2]. BI-113823 (1 μM) inhibited DBK-induced upregulation of B1R and activation of the PI3K/Akt and ERK signaling pathways in human hepatic stellate cell line LX2 [2].
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| ln Vivo |
BI-113823 (1-30 mg/kg; oral; single dose; 1-10 nM; intrathecal injection; single dose; 2.6 mg/kg; intravenous injection; single dose; 3.7 mg/kg/h; continuous intravenous infusion) dose-dependently relieved CFA-induced mechanosensitive hyperalgesia, reducing mechanosensitivity of peripheral afferent nerves in rats to 45% of baseline at maximum effect [1]. BI-113823 (50 mg/kg; oral; once daily; for 6 weeks) reduced CCl4 and bile duct ligation (BDL)-induced liver fibrosis and portal hypertension, and downregulated profibrotic and inflammatory mediators by inhibiting the Akt signaling pathway [2].
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| Cell Assay |
Immunofluorescence [2]
Cell Types: LX2 human hepatic stellate cells (hHSCs) Tested Concentrations: 1 μM Incubation Duration: 24 hours Experimental Results: Immunofluorescence images showed that TGF-β-induced α-SMA expression was strongly inhibited, as evidenced by a decrease in red fluorescence intensity. Western Blot Analysis [2] Cell Types: LX2 human hepatic stellate cells (hHSCs) Tested Concentrations: 0, 1, 2 μM Incubation Duration: 24 hours Experimental Results: Reduced the expression of TGF-β-stimulated profibrotic proteins (α-SMA, Col-1, VEGF, MCP-1) and B1R. Inhibited TGF-β-induced Akt phosphorylation. Cell migration assay [2] Cell Types: LX2 human hepatic stellate cells (hHSCs) Tested Concentrations: 0.1 μM, 1 μM Incubation Duration: 12 hours Experimental Results: Compared with 1% FBS alone (~75%), the migration rate of 1% FBS stimulation at 0.1 μM decreased to about 50%, and at 1 μM it decreased to about 35%. |
| Animal Protocol |
Animal/Disease Models:Han-Wistar mice (male, 200-420 g, CFA-induced inflammatory pain model) [1]
Doses: 1-30 mg/kg (oral); 1-10 nM (injection)/2.6 mg/kg (intravenous bolus); 3.7 mg/kg/h (intravenous maintenance infusion) Route of Administration: Oral; single dose; injection; single/intravenous; bolus; maintenance infusion Experimental Results: Reduced CFA-induced mechanical hyperalgesia in a dose-dependent manner. The effect of oral administration of 30 mg/kg was comparable to that of oral administration of 30 mg/kg indomethacin. Reversed CFA-induced hyperalgesia in a dose-dependent manner. A concentration of 10 nM was sufficient to completely reverse hyperalgesia, with an effect comparable to that of intrathecal morphine of 20 nM. In CFA-treated rats, the drug reduced the firing frequency of peripheral afferent nerves to 45% of baseline, with the maximum effect reached 30 minutes after administration. Animal/Disease Models:BALB/c (male, 8-10 weeks old, 25-30 g, injected with CCl4 twice a week for 6 weeks to induce liver fibrosis) [2] Doses: 50 mg/kg Route of Administration: Oral; once daily; for 6 weeks Experimental Results: Significantly reduced Sirius red positive collagen area, liver hydroxyproline content and α-SMA expression. Significantly reduced liver/body weight ratio and portal vein pressure. Survival rate increased to 75% (15 out of 20 mice survived, compared to only 10 out of 22 mice in the vector control group). Significantly reduced mRNA and protein expression of profibrotic mediators α-SMA, collagen I, collagen III, collagen IV, PDGF, TGFβ, CTGF, VEGF and PCNA in the liver. Reduced Akt phosphorylation level in the liver. The expression of inflammatory cytokines IL-1β and IL-6, chemokines MCP-1, MCP-3, and TIMP-1, as well as inflammatory cell markers CD68, neutrophil elastase, and COX-2 in the liver were significantly reduced. Macrophage and neutrophil infiltration was decreased. |
| References |
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| CAS # |
1119282-90-4
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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.) |
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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