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-P3061
    [Hyp3]-Bradykinin
    		Agonist 99.73%
    [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-168906
    BI-113823
    		Antagonist 99.23%
    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.
    BI-113823
  • HY-15043
    ELN-441958
    		Antagonist 99.17%
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse.
    ELN-441958
  • HY-P4676
    Lys-(Des-Arg9,Leu8)-Bradykinin
    		Antagonist 98.23%
    Lys-(Des-Arg9,Leu8)-Bradykinin is a selective bradykinin B1 receptor (BDKRB1) antagonist. Lys-(Des-Arg9,Leu8)-Bradykinin inhibits local inflammatory edema. Lys-(Des-Arg9,Leu8)-Bradykinin induces the production of systemic acute-phase proteins. Lys-(Des-Arg9,Leu8)-Bradykinin is applicable to research related to peptidoglycan-polysaccharide-induced acute arthritis.
    Lys-(Des-Arg9,Leu8)-Bradykinin
  • 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-P0206F
    biotin-Bradykinin
    		Modulator 99.93%
    biotin-Bradykinin is a biological active peptide. (Biotin labeled HY-P0206)
    biotin-Bradykinin
  • HY-103289
    MEN 11270
    		Antagonist 99.15%
    MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with a pKi value of 10.3.
    MEN 11270
  • HY-P3209
    Des-Arg9-[Leu8]-Bradykinin acetate
    		Inhibitor 98.36%
    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-121156
    Anatibant
    		Antagonist
    Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases.
    Anatibant
  • HY-100827
    Safotibant
    		Antagonist 98.88%
    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
  • HY-P1490
    Bradykinin (2-9)
    		Modulator
    Bradykinin (2-9) is an amino-truncated Bradykinin peptide. Bradykinin (2-9) is a metabolite of Bradykinin, cleaved by Aminopeptidase P.
    Bradykinin (2-9)
  • HY-P5518A
    [Des-Arg10]-HOE I40 TFA
    		Antagonist 99.84%
    [Des-Arg10]-HOE I40 TFA is a potent bradykinin B1 receptor antagonist.
    [Des-Arg10]-HOE I40 TFA
  • HY-108896R
    Icatibant acetate (Standard)
    		Antagonist
    Icatibant (acetate) (Standard) is the analytical standard of Icatibant (acetate). This product is intended for research and analytical applications. Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively.
    Icatibant acetate (Standard)
  • 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-P0206S1
    RPP-(Gly-13C2,15N)-FSPFR TFA
    RPP-(Gly-113C2,15N)-FSPFR TFA is 13C- and 15N-labeled Bradykinin (HY-P0206). Bradykinin is an effective endothelium-dependent vasodilator that can lower blood pressure. Bradykinin can induce contraction of bronchial and intestinal non-vascular smooth muscle, increase vascular permeability, and participate in the mechanism of pain.
    RPP-(Gly-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N)-FSPFR TFA
  • 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-P3543
    T-kinin
    T-kinin (Ile-Ser-bradykinin) is a peptide containing bradykinin. T-kinin can be used for the research of inflammation.
    T-kinin
  • HY-P3232
    B 9430
    		Antagonist
    B 9430 is a potent bradykinin B1/B2 receptor antagonist.
    B 9430
  • HY-15042
    MK 0686
    		99.76%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Bradykinin Receptor Isoform Comparison

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