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 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.
    Bradykinin
  • HY-17446
    Icatibant
    		Antagonist 99.63%
    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-P0298A
    [Des-Arg9]-Bradykinin acetate
    		Agonist 99.95%
    [Des-Arg9]-Bradykinin acetate is a Bradykinin B1 receptor agonist that displays selectivity for B1 over B2 receptors.
    [Des-Arg9]-Bradykinin 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-121156A
    Anatibant hydrochloride
    		Antagonist
    Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride 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 hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases.
    Anatibant hydrochloride
  • 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-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-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-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-103293A
    Lys-Bradykinin TFA
    		Agonist 99.44%
    Lys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation.
    Lys-Bradykinin TFA
  • HY-147273
    Fulimetibant
    		Antagonist 99.74%
    Fulimetibant is a bradykinin receptor antagonist.
    Fulimetibant
  • 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-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-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-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-103291
    Sar-[D-Phe8]-des-Arg9-Bradykinin
    		Agonist 99.34%
    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 99.38%
    Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE).
    Bradykinin (1-5)
  • HY-P1484
    Bradykinin (1-7)
    		Modulator 99.59%
    Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase.
    Bradykinin (1-7)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Bradykinin Receptor Isoform Comparison

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