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 (36):

Cat. No. Product Name Effect Purity
  • 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-P0206
    Bradykinin Modulator 99.86%
    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-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-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[1][2][3].
  • HY-108896
    Icatibant acetate Antagonist 99.65%
    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[1][2][3].
  • 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-P0298
    [Des-Arg9]-Bradykinin Agonist
    [Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors.
  • HY-P3232
    B 9430 Antagonist
    B 9430 is a potent bradykinin B1/B2 receptor antagonist[1].
  • HY-103290
    R715 Antagonist 99.45%
    R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice[1].
  • HY-103291
    Sar-[D-Phe8]-des-Arg9-Bradykinin Agonist
    Sar-[D-Phe8]-des-Arg9-Bradykinin is a agonist of B1 receptor. Sar-[D-Phe8]-des-Arg9-Bradykinin selectively amplifies the contractile response when incubation with human recombinant interleukin-1 β (IL-1 β) in rabbit aortic rings[1].
  • HY-147273
    Fulimetibant Antagonist 99.74%
    Fulimetibant is a bradykinin receptor antagonist[1].
  • 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[1].
  • 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-P1488
    Bradykinin (1-5) Modulator
    Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE).
  • 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[1][2].
  • HY-105155
    Lobradimil Agonist 99.51%
    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[1].
  • HY-103295A
    Lys-[Des-Arg9]Bradykinin TFA Agonist 99.43%
    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[1][2].
  • HY-P4676
    Lys-(Des-Arg9,Leu8)-Bradykinin Antagonist
    Lys-(Des-Arg9,Leu8)-Bradykinin is a bradykinin B1 receptor antagonist[1].
  • 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. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation[1].
  • 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[1].