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

Bradykinin Receptor

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 Related Products (27):

Cat. No. Product Name Effect Purity
  • HY-P0206
    Bradykinin
    Modulator 99.92%
    Bradykinin is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions.
  • HY-17446
    Icatibant
    Antagonist 99.51%
    Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
  • HY-108896
    Icatibant acetate
    Antagonist 99.64%
    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.
  • HY-15039
    SSR240612
    Antagonist 99.51%
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
  • HY-P0298A
    [Des-Arg9]-Bradykinin acetate
    Agonist 99.92%
    [Des-Arg9]-Bradykinin acetate is a Bradykinin B1 receptor agonist that displays selectivity for B1 over B2 receptors.
  • HY-147273
    Fulimetibant
    Antagonist
    Fulimetibant is a bradykinin receptor antagonist.
  • HY-P3232
    B 9430
    Antagonist
    B 9430 is a potent bradykinin B1/B2 receptor antagonist.
  • HY-105155
    Lobradimil
    Agonist
    Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors.
  • HY-103295A
    Lys-[Des-Arg9]Bradykinin TFA
    Agonist 99.48%
    Lys-[Des-Arg9]Bradykinin TFA, 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 TFA has low inhibitory activity on B2 receptors.
  • HY-15043
    ELN-441958
    Antagonist 99.84%
    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.
  • HY-P1488
    Bradykinin (1-5)
    Modulator ≥99.0%
    Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE).
  • HY-P1484
    Bradykinin (1-7)
    Modulator 99.87%
    Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase.
  • HY-P1490
    Bradykinin (2-9)
    Modulator 99.94%
    Bradykinin (2-9) is an amino-truncated Bradykinin peptide. Bradykinin (2-9) is a metabolite of Bradykinin, cleaved by Aminopeptidase P.
  • HY-P0298
    [Des-Arg9]-Bradykinin
    Agonist
    [Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors.
  • HY-P1469
    Bradykinin (1-6)
    Modulator 98.95%
    Bradykinin (1-6) is an amino-truncated Bradykinin peptide. Bradykinin (1-6) is a stable metabolite of Bradykinin, cleaved by carboxypeptidase Y (CPY).
  • HY-145562
    Deucrictibant
    Antagonist
    Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family.
  • 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.
  • HY-106277A
    Fasitibant chloride hydrochloride
    Inhibitor
    Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and longlasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis, et al.
  • 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.
  • HY-P3061
    [Hyp3]-Bradykinin
    Agonist
    [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.