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 Isoform Specific Products
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Bradykinin Receptor Related Products (70)
Related Products (70)
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Antibodies (1)
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Bradykinin Receptor Isoform Comparison
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BI-113823
0 ImagesBI-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.
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ELN-441958
0 ImagesELN-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.
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[Des-Arg9]-Bradykinin
![[Des-Arg9]-Bradykinin](https://file.medchemexpress.com/product_pic/hy-p0298.gif "Click to View [Des-Arg9]-Bradykinin Product Detail")
0 ImagesCat. No.: HY-P0298CAS No.: 15958-92-6[Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors.
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biotin-Bradykinin
0 Imagesbiotin-Bradykinin is a biological active peptide. (Biotin labeled HY-P0206)
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MEN 11270
0 ImagesMEN 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.
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Des-Arg9-[Leu8]-Bradykinin acetate
![Des-Arg9-[Leu8]-Bradykinin acetate](https://file.medchemexpress.com/product_pic/hy-p3209.gif "Click to View Des-Arg9-[Leu8]-Bradykinin acetate Product Detail")
0 ImagesDes-Arg9-[Leu8]-Bradykinin acetate is potent bradykinin receptor 1 (B1R) antagonist. Des-Arg9-[Leu8]-Bradykinin acetate can be used for renal fibrosis research.
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Anatibant
0 ImagesCat. No.: HY-121156CAS No.: 209733-45-9Synonyms: LF 16-0687; XY-2405Anatibant (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.
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Safotibant
0 ImagesSynonyms: LF22-0542Safotibant (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.
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Bradykinin (2-9)
0 ImagesCat. No.: HY-P1490CAS No.: 16875-11-9Synonyms: Des-Arg1-bradykininBradykinin (2-9) is an amino-truncated Bradykinin peptide. Bradykinin (2-9) is a metabolite of Bradykinin, cleaved by Aminopeptidase P.
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FR173657
0 ImagesCat. No.: HY-15791CAS No.: 167838-64-4Synonyms: FK-3657FR173657 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.
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[Des-Arg10]-HOE I40 TFA
![[Des-Arg10]-HOE I40 TFA](https://file.medchemexpress.com/product_pic/hy-p5518a.gif "Click to View [Des-Arg10]-HOE I40 TFA Product Detail")
0 ImagesCat. No.: HY-P5518APurity: 99.84%[Des-Arg10]-HOE I40 TFA is a potent bradykinin B1 receptor antagonist.
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WIN 64338 hydrochloride
0 ImagesWIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM).
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Icatibant acetate (Standard)
0 ImagesSynonyms: HOE 140 acetate (Standard)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.
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Fasitibant free base
0 ImagesCat. No.: HY-106277CAS No.: 869939-83-3Fasitibant (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.
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RPP-(Gly-13C2,15N)-FSPFR TFA
0 ImagesCat. No.: HY-P0206S1RPP-(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.
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Bradykinin (1-3)
0 ImagesCat. No.: HY-P1497CAS No.: 23815-91-0Bradykinin (1-3) is a 3-amino acid residue peptide. Bradykinin (1-3) is an amino-truncated Bradykinin peptide, cleaved by Prolyl endopeptidase.
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T-kinin
0 ImagesCat. No.: HY-P3543CAS No.: 86030-63-9Synonyms: Ile-Ser-bradykininT-kinin (Ile-Ser-bradykinin) is a peptide containing bradykinin. T-kinin can be used for the research of inflammation.
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B 9430
0 ImagesCat. No.: HY-P3232CAS No.: 180981-09-3B 9430 is a potent bradykinin B1/B2 receptor antagonist.
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MK 0686
0 ImagesMK 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.
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Fasitibant chloride hydrochloride
0 ImagesCat. No.: HY-106277ACAS No.: 869880-33-1Synonyms: MEN16132Fasitibant 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.
