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-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.
    Bradykinin
  • 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.
    Icatibant
  • 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.
    Icatibant acetate
  • 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.
    SSR240612
  • 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.
    Lobradimil
  • 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.
    R715
  • HY-15791
    FR173657
    		Antagonist
    FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease.
    FR173657
  • 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.
    Lys-[Des-Arg9]Bradykinin TFA
  • 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.
    [Des-Arg9]-Bradykinin acetate
  • 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-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.
    Bradykinin (1-7)
  • HY-147273
    Fulimetibant
    		Antagonist 99.74%
    Fulimetibant is a bradykinin receptor antagonist.
    Fulimetibant
  • HY-15043
    ELN-441958
    		Antagonist 99.51%
    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-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-P3751
    [Tyr8] Bradykinin
    		Agonist 99.61%
    [Tyr8] Bradykinin is a B2 kinin receptor agonist. [Tyr8] Bradykinin also stimulates ERK1/2 phosphorylation. [Tyr8] Bradykinin can be used as an internal standard.
    [Tyr8] 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-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.
    Sar-[D-Phe8]-des-Arg9-Bradykinin
  • 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).
    Bradykinin (1-5)
  • HY-P1469
    Bradykinin (1-6)
    		Modulator 99.19%
    Bradykinin (1-6) is an amino-truncated Bradykinin peptide. Bradykinin (1-6) is a stable metabolite of Bradykinin, cleaved by carboxypeptidase Y (CPY).
    Bradykinin (1-6)
  • 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
Bradykinin Receptor Isoform Comparison

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