2. Signaling Pathways
  3. GPCR/G Protein
  4. Bradykinin Receptor

Bradykinin Receptor

Bradykinin Receptor

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Bradykinin receptors are cell surface, G protein-coupled receptor (GPCR) family members. There are two subtypes of bradykinin receptors, B1 and B2. Bradykinin receptor-mediated signal transductions play a significant role in maintaining cardiovascular homeostasis, regulating pain and inflammation. Both receptors transduce extracellular signals through the activation of G-proteins.

Bradykinin B1 receptor is expressed at a very low level in healthy tissues, but is induced under stressful conditions such as shock or inflammation, whereas the bradykinin B2 receptor is ubiquitous and is constitutively expressed. Bradykinin B2 receptor is involved in vasodilation, osmoregulation, smooth muscle contraction, and nociceptor activation. Bradykinin B1 receptor and Bradykinin B2 receptor have emerged as therapeutic targets as they are implicated in inflammatory disease, vasculopathy, neuropathy, obesity, diabetes, and cancer. B1R and B2R can hold dichotomous roles in diseases. Agonists and antagonists have been evaluated as therapeutics.

Bradykinin Receptor Isoform Specific Products:

Bradykinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0298
    [Des-Arg9]-Bradykinin
    		Agonist
    [Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors.
    [Des-Arg9]-Bradykinin
  • HY-P4676
    Lys-(Des-Arg9,Leu8)-Bradykinin
    		Antagonist 98.23%
    Lys-(Des-Arg9,Leu8)-Bradykinin is a bradykinin B1 receptor antagonist.
    Lys-(Des-Arg9,Leu8)-Bradykinin
  • HY-P3061
    [Hyp3]-Bradykinin
    		Agonist 99.01%
    [Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts.
    [Hyp3]-Bradykinin
  • HY-P0206A
    Bradykinin acetate
    		Modulator
    Bradykinin acetate is an effective endothelium-dependent vasodilator that can lower blood pressure. Bradykinin acetate can induce contraction of bronchial and intestinal non-vascular smooth muscle, increase vascular permeability, and participate in the mechanism of pain.
    Bradykinin acetate
  • HY-106277
    Fasitibant free base
    		Antagonist
    Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.
    Fasitibant free base
  • HY-P1497
    Bradykinin (1-3)
    		Modulator
    Bradykinin (1-3) is a 3-amino acid residue peptide. Bradykinin (1-3) is an amino-truncated Bradykinin peptide, cleaved by Prolyl endopeptidase.
    Bradykinin (1-3)
  • HY-P3232
    B 9430
    		Antagonist
    B 9430 is a potent bradykinin B1/B2 receptor antagonist.
    B 9430
  • HY-15042
    MK 0686
    MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time.
    MK 0686
  • HY-106277A
    Fasitibant chloride hydrochloride
    		Antagonist
    Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.
    Fasitibant chloride hydrochloride
  • HY-100301
    FR167344 free base
    		Antagonist
    FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
    FR167344 free base
  • HY-103295
    Lys-[Des-Arg9]Bradykinin
    		Agonist
    Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors.
    Lys-[Des-Arg9]Bradykinin
  • HY-123376
    FR-190997
    		Agonist
    FR-190997 is a non-peptide Bradykinin B2 receptor selective agonist, Ki value is 9.8 nM. FR-190997 is also an effective antihypertensive agent.
    FR-190997
  • HY-P1694
    B4148
    		Antagonist
    B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group.
    B4148
  • HY-103293
    Lys-Bradykinin
    		Agonist
    Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation.
    Lys-Bradykinin
  • HY-P3544
    Lys-[Hyp3]-Bradykinin
    		Agonist
    Lys-[Hyp3]-Bradykinin a Bradykinin (HY-P0206) agonist. Lys-[Hyp3]-Bradykinin is a kinin, it can be isolated from human urine. Lys-[Hyp3]-Bradykinin can be used for the research of inflammation.
    Lys-[Hyp3]-Bradykinin
  • HY-P3209
    Des-Arg9-[Leu8]-Bradykinin acetate
    		Inhibitor
    Des-Arg9-[Leu8]-Bradykinin acetate is potent bradykinin receptor 1 (B1R) antagonist. Des-Arg9-[Leu8]-Bradykinin acetate can be used for renal fibrosis research.
    Des-Arg9-[Leu8]-Bradykinin acetate
  • HY-P2109
    JMV-1645
    		Antagonist
    JMV-1645 is a potent and selective B1 bradykinin receptor antagonist with a Ki value of 0.023 nM on the human cloned B1 receptor. JMV-1645 can be utilized in trauma and infection research.
    JMV-1645
  • HY-P3750
    Methionyl-Lysyl-Bradykinin
    		Agonist
    Methionyl-Lysyl-Bradykinin (Met-Lys-Bradykinin), a Bradykinin (HY-P0206) analogue, is a kinin.
    Methionyl-Lysyl-Bradykinin
  • HY-158262
    Bradykinin B1 receptor antagonist 1
    		Antagonist
    Bradykinin B1 receptor antagonist 1 (compound 6B) is a potent and cross the blood-brain barrier bradykinin B1 antagonist. Bradykinin B1 receptor antagonist 1 has the potential for the research of pain.
    Bradykinin B1 receptor antagonist 1
  • HY-100827
    Safotibant
    		Antagonist
    Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model.
    Safotibant
Cat. No. Product Name / Synonyms Application Reactivity
Bradykinin Receptor Isoform Comparison

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