BI-113823
Based on 1 Customer Validation
BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
The BI-113823 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Reinheit: 99.23%
- CAS. Nr.: 1119282-90-4
- Formel: C26H44N4O5S
- Molecular Weight:524.72
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
BI-113823 (10-7-10-6 M; 12 h) inhibits TNF-α-induced migration of human peripheral blood monocytes and human peripheral blood neutrophils in a dose-dependent manner[2].
BI-113823 (10-7-10-6 M) reduces LPS (HY-D1056)-induced TNF-α production in human peripheral blood mononuclear cells in a dose-dependent manner[2].
BI-113823 (10-100 nM) inhibits LPS-induced activation of human peripheral blood monocytes and human peripheral blood neutrophils, and reduces the expression level of CD11/CD18[2].
BI-113823 (10-7-10-6 M) reduces LPS-induced MPO activity in human peripheral blood neutrophils in a dose-dependent manner[2].
BI-113823 (1 μM; 24 h) inhibits TGF-β-induced α-SMA expression in LX2 human hepatic stellate cells[2].
BI-113823 (0-2 μM; 24 h) reduces the expression of TGF-β-stimulated profibrotic proteins and B1R, and inhibits the phosphorylation of Akt in human hepatic stellate cell line LX2[2].
BI-113823 (0.1-1 μM; 0-48 h) dose-dependently inhibits TGF-β-induced contraction of LX2 human hepatic stellate cells in collagen gels[2].
BI-113823 (0.1-1 μM; 12 h) inhibits the migration of 1% FBS-stimulated human hepatic stellate cell line LX2 in a dose-dependent manner[2].
BI-113823 (0.1-2 μM) inhibits DBK (HY-P0298)-induced scratch wound healing migration of human hepatic stellate cell line LX2 in a dose-dependent manner[2].
BI-113823 (0.001-1 μM) inhibits DBK-stimulated proliferation of human hepatic stellate cell line LX2 in a dose-dependent manner, without affecting baseline proliferation or inducing apoptosis[2].
BI-113823 (1 μM) inhibits G1-to-S phase cell cycle transition in human hepatic stellate cell line LX2 stimulated by DBK[2].
BI-113823 (1 μM) inhibits DBK-induced upregulation of B1R and activation of the PI3K/Akt and ERK signaling pathways in human hepatic stellate cell line LX2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LX2 human hepatic stellate cells (hHSCs)
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Concentration:1 μM
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Incubation Time:24 h
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Result:Strongly inhibited TGF-β-induced α-SMA expression, as shown by reduced red fluorescence intensity in immunofluorescence images.
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Cell Line:LX2 human hepatic stellate cells (hHSCs)
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Concentration:0, 1, 2 μM
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Incubation Time:24 h
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Result:Reduced TGF-β-stimulated expression of profibrotic proteins (α-SMA, Col-1, VEGF, MCP-1) and B1Rs.
Inhibited TGF-β-induced phosphorylation of Akt.
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Cell Line:LX2 human hepatic stellate cells (hHSCs)
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Concentration:0.1 μM, 1 μM
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Incubation Time:12 h
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Result:Reduced 1% FBS-stimulated migration to ~50% at 0.1 μM and ~35% at 1 μM, compared to 1% FBS alone (~75%).
BI-113823 (50 mg/kg; p.o.; once daily; for 6 consecutive weeks) alleviates liver fibrosis and portal hypertension induced by CCl4 (HY-Y0298) and bile duct ligation (BDL), and downregulates profibrotic and inflammatory mediators by inhibiting the Akt signaling pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Han-Wistar (male, 200-420 g, CFA-induced inflammatory pain model)[1]
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Dosage:1-30 mg/kg (p.o.); 1-10 nM (i.t.)/2.6 mg/kg (i.v. bolus); 3.7 mg/kg/h (i.v. maintenance infusion)
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Administration:p.o.; single dose; i.t.; single dose/i.v.; bolus injection; maintenance infusion
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Result:Reduced CFA-induced mechanical hyperalgesia in a dose-dependent manner.
Produced an effect comparable to 30 mg/kg oral indomethacin at 30 mg/kg p.o.
Reversed CFA-induced hyperalgesia in a dose-dependent manner.
Completely reversed hyperalgesia at 10 nM i.t., an effect comparable to 20 nM intrathecal morphine.
Reduced the firing rate of peripheral afferents in CFA-treated rats to up to 45% of baseline, with maximum effect reached 30 min after start of administration.
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Animal Model:BALB/c (male, 8-10 weeks old, 25-30 g, hepatic fibrosis induced by CCl4 injection twice weekly for 6 weeks)[2]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 6 weeks
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Result:Significantly reduced sirius red-positive collagen area, hepatic hydroxyproline content, and α-SMA expression.
Significantly decreased liver/body weight ratio and portal vein pressure.
Improved survival to 75% (15/20 mice survived, compared to 10/22 in vehicle-treated mice).
Significantly reduced hepatic mRNA and protein expression of profibrotic mediators α-SMA, collagen 1, collagen 3, collagen 4, PDGF, TGFβ, CTGF, VEGF, and PCNA.
Reduced hepatic Akt phosphorylation.
Significantly reduced hepatic expression of inflammatory cytokines IL-1β, IL-6, chemokines MCP-1, MCP-3, TIMP-1, and inflammatory cell markers CD68, neutrophil elastase, COX-2.
Reduced infiltration of macrophages and neutrophils.
Chemical Information
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CAS. Nr. 1119282-90-4
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Appearance Oil
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Molecular Weight 524.72
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Formel C26H44N4O5S
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Color Colorless to light yellow
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SMILES
O=S(N(C)CCOCC(N([C@@H]1C[C@H](N2CCN(CC2)C)CCC1)C)=O)(C3=C(C=C(C=C3C)OC)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (190.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Schuelert N, et al. The bradykinin B1 receptor antagonist BI113823 reverses inflammatory hyperalgesia by desensitization of peripheral and spinal neurons. Eur J Pain. 2015;19(1):132-142. [Content Brief]
[2]. Rampa DR, et al. Kinin B1 receptor blockade attenuates hepatic fibrosis and portal hypertension in chronic liver diseases in mice. J Transl Med. 2022;20(1):590. Published 2022 Dec 13. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9058 mL | 9.5289 mL | 19.0578 mL | 47.6445 mL |
| 5 mM | 0.3812 mL | 1.9058 mL | 3.8116 mL | 9.5289 mL | |
| 10 mM | 0.1906 mL | 0.9529 mL | 1.9058 mL | 4.7644 mL | |
| 15 mM | 0.1271 mL | 0.6353 mL | 1.2705 mL | 3.1763 mL | |
| 20 mM | 0.0953 mL | 0.4764 mL | 0.9529 mL | 2.3822 mL | |
| 25 mM | 0.0762 mL | 0.3812 mL | 0.7623 mL | 1.9058 mL | |
| 30 mM | 0.0635 mL | 0.3176 mL | 0.6353 mL | 1.5881 mL | |
| 40 mM | 0.0476 mL | 0.2382 mL | 0.4764 mL | 1.1911 mL | |
| 50 mM | 0.0381 mL | 0.1906 mL | 0.3812 mL | 0.9529 mL | |
| 60 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7941 mL | |
| 80 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5956 mL | |
| 100 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.4764 mL |
BI-113823 Related Classifications
HY-168906 Related Classifications
Powered by Bioz
- BI-113823
- 1119282-90-4
- BI113823
- BI 113823
- Bradykinin Receptor
- PI3K
- Akt
- TNF Receptor
- ERK
- human peripheral blood neutrophils
- LX2 human hepatic stellate cells
- human peripheral blood monocytes
- inflammatory pain
- bradykinin B1 receptor
- portal hypertension
- PI3K/Akt signaling
- spinal nociceptive-specific neurons
- hepatic fibrosis
- ERK signalling pathways
- Inhibitor
- inhibitor
- inhibit