2. GPCR/G Protein PI3K/Akt/mTOR Apoptosis MAPK/ERK Pathway Stem Cell/Wnt
  3. Bradykinin Receptor PI3K Akt TNF Receptor ERK
  4. BI-113823

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.

For research use only. We do not sell to patients.

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.

BI-113823

BI-113823 Chemical Structure

CAS No. : 1119282-90-4

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Based on 1 publication(s) in Google Scholar

BI-113823 Related Antibodies

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Bradykinin B1 Receptor (B1R) Bradykinin B2 Receptor (B2R)

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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ERK ERK1 ERK2 ERK5 ERK8

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Description

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[1][2].

In Vitro

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.

BI-113823 Related Antibodies

Immunofluorescence[2]

Cell Line: LX2 human hepatic stellate cells (hHSCs)
Concentration: 1 μM
Incubation Time: 24 h
Result: Strongly inhibited TGF-β-induced α-SMA expression, as shown by reduced red fluorescence intensity in immunofluorescence images.

Western Blot Analysis[2]

Cell Line: LX2 human hepatic stellate cells (hHSCs)
Concentration: 0, 1, 2 μM
Incubation Time: 24 h
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.

Cell Migration Assay [2]

Cell Line: LX2 human hepatic stellate cells (hHSCs)
Concentration: 0.1 μM, 1 μM
Incubation Time: 12 h
Result: Reduced 1% FBS-stimulated migration to ~50% at 0.1 μM and ~35% at 1 μM, compared to 1% FBS alone (~75%).
In Vivo

BI-113823 (1-30 mg/kg; p.o.; single administration; 1-10 nM; intrathecal injection; single administration; 2.6 mg/kg; i.v.; single administration; 3.7 mg/kg/h; i.v.; continuous infusion) dose-dependently alleviates CFA (HY-153808)-induced mechanical hyperalgesia, reducing the mechanical sensitivity of peripheral afferent nerves in rats to 45% of the baseline level at its maximal effect[1].
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.

Animal Model: Han-Wistar (male, 200-420 g, CFA-induced inflammatory pain model)[1]
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)
Administration: p.o.; single dose; i.t.; single dose/i.v.; bolus injection; maintenance infusion
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.
Animal Model: BALB/c (male, 8-10 weeks old, 25-30 g, hepatic fibrosis induced by CCl4 injection twice weekly for 6 weeks)[2]
Dosage: 50 mg/kg
Administration: p.o.; daily; 6 weeks
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.
Molecular Weight

524.72

Formula

C26H44N4O5S
CAS No.
Appearance

Oil

Color

Colorless to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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BI-113823 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI-1138231119282-90-4BI113823BI 113823Bradykinin ReceptorPI3KAktTNF ReceptorERKPhosphoinositide 3-kinasePKBProtein kinase BTumor Necrosis Factor ReceptorTNFRExtracellular signal regulated kinaseshuman peripheral blood neutrophilsLX2 human hepatic stellate cellshuman peripheral blood monocytesinflammatory painbradykinin B1 receptorportal hypertensionPI3K/Akt signalingspinal nociceptive-specific neuronshepatic fibrosisERK signalling pathwaysInhibitorinhibitorinhibit

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