Bradykinin Receptor

Bradykinin receptor agonists and antagonists act on B1 and B2, two G protein-coupled kinin receptors. Kinin peptides such as bradykinin are released from kininogens by kallikreins and regulate vascular tone, permeability and pain signaling. The B2 receptor is expressed constitutively in many tissues, and the human receptor was cloned in 1992. The B1 receptor, cloned in 1994, is induced by tissue injury and inflammation and prefers des-Arg kinin metabolites. A 2005 International Union of Pharmacology (IUPHAR) review set out this classification of the kinin receptor family. Icatibant is a peptide B2 antagonist, and FR167344 free base is a nonpeptide B2 antagonist. R715 and SSR240612 block the B1 receptor, while Lys-[Des-Arg9]Bradykinin TFA acts as a B1 agonist.

22 Items

  • SSR240612
    Cat. No.
    A13839

    SSR240612

    SSR240612 is a new antagonist of the bradykinin B1 receptor.

    1 mg
    $220.00
    2 mg
    $350.00
    All 8 sizes
  • FR167344 free base
    Cat. No.
    A12964

    FR167344 free base

    Synonyms: FR 167344

    FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist.

    1 mg
    $1,080.00
    5 mg
    $3,240.00
    All 4 sizes
  • Icatibant
    Cat. No.
    A18074

    Icatibant

    Synonyms: Firazyr

    Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.

    500 µg
    $150.00
    1 mg
    $245.00
    All 4 sizes
  • ELN-441958
    Cat. No.
    A21207

    ELN-441958

    ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM.

    1 mg
    $50.00
    5 mg
    $130.00
    All 7 sizes
  • R715
    Cat. No.
    A23883

    R715

    R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin-diabetic mice.

    1 mg
    $295.00
    5 mg
    $745.00
    All 3 sizes
  • WIN 64338
    Cat. No.
    A59123

    WIN 64338

    WIN 64338 is a non-peptide antagonist of the bradykinin B2 receptor. It effectively inhibits bradykinin-evoked trigeminal nerve stimulation, making it valuable for research related to pain signaling pathways and inflammatory responses. This compound is relevant for studies investigating the role of bradykinin in various physiological and pathological states.

    Out of stock

    All 3 sizes
  • Anatibant hydrochloride
    Cat. No.
    A59127

    Anatibant hydrochloride

    Synonyms: LF 16-0687 hydrochloride; XY-2405 hydrochloride

    Anatibant hydrochloride is a selective non-peptide antagonist of the bradykinin B2 receptor. It exhibits high affinity binding to recombinant B2 receptors in human, rat, and guinea pig models, with Ki values of 0.67 nM, 1.74 nM, and 1.37 nM, respectively. Notably, Anatibant hydrochloride is capable of crossing the blood-brain barrier, making it a valuable tool for investigating pathophysiological conditions related to brain injury and neuroinflammation.

    1 mg
    $280.00
    5 mg
    $675.00
    All 4 sizes
  • Fulimetibant
    Cat. No.
    A59131

    Fulimetibant

    Fulimetibant is a selective antagonist of bradykinin receptors, primarily B1 and B2 subtypes. This compound inhibits the action of bradykinin, a peptide involved in pain and inflammatory responses. Fulimetibant is utilized in research to investigate the role of bradykinin in various pathological conditions, including pain mechanisms and inflammation-related disorders.

    5 mg
    $335.00
    10 mg
    $565.00
    All 5 sizes
  • Lys-(Des-Arg9,Leu8)-Bradykinin
    Cat. No.
    A59132

    Lys-(Des-Arg9,Leu8)-Bradykinin

    Lys-(Des-Arg9,Leu8)-Bradykinin is a selective antagonist of the bradykinin B1 receptor. This compound inhibits bradykinin-mediated signaling pathways, making it valuable for studies focused on pain, inflammation, and vascular permeability. Its role in various experimental models facilitates the investigation of bradykinin's effects on physiological and pathological conditions.

    1 mg
    $30.00
    5 mg
    $60.00
    All 3 sizes
  • BI-113823
    Cat. No.
    A59133

    BI-113823

    BI-113823 is a selective antagonist of the bradykinin B1 receptor, exhibiting oral bioactivity. It effectively alleviates mechanical hyperalgesia induced by complete Freund's adjuvant in animal models. This compound is relevant for research focused on chronic inflammatory pain mechanisms and potential therapeutic strategies.

    5 mg
    $615.00
    10 mg
    $1,010.00
    All 5 sizes
  • Anatibant
    Cat. No.
    A59137

    Anatibant

    Synonyms: LF 16-0687; XY-2405

    Anatibant is a selective non-peptide antagonist of the bradykinin B2 receptor. It demonstrates high affinity for recombinant human, rat, and guinea-pig B2 receptors, with Ki values of 0.67 nM, 1.74 nM, and 1.37 nM, respectively. This compound effectively crosses the blood-brain barrier, making it a valuable tool for investigating the role of bradykinin signaling in brain damage diseases and related neuroinflammatory conditions.

    25 mg
    $1,405.00
    50 mg
    $1,790.00
    All 3 sizes
  • Fasitibant free base
    Cat. No.
    A59139

    Fasitibant free base

    Fasitibant free base is a selective antagonist of the bradykinin B2 receptor, exhibiting high affinity and prolonged activity. This compound is primarily utilized in research focused on inflammatory pathways, particularly in the study of osteoarthritis and rheumatoid arthritis. Its ability to modulate proinflammatory responses makes it a valuable tool for investigating therapeutic approaches targeting these conditions.

    25 mg
    $2,160.00
    50 mg
    $2,770.00
    All 3 sizes
  • B 9430
    Cat. No.
    A59142

    B 9430

    B 9430 is a potent antagonist of both bradykinin B1 and B2 receptors. By inhibiting these receptors, B 9430 plays a crucial role in modulating inflammatory responses and pain signaling pathways. This compound is applicable in research focused on cardiovascular diseases, pain management, and various inflammatory conditions.

    Out of stock

    All 3 sizes
  • Fasitibant chloride hydrochloride
    Cat. No.
    A59144

    Fasitibant chloride hydrochloride

    Synonyms: MEN16132

    Fasitibant chloride hydrochloride is a selective and high-affinity antagonist of the bradykinin B2 receptor, exhibiting potent and long-lasting activity. This compound is specifically investigated for its proinflammatory effects and is valuable in research focused on osteoarthritis and rheumatoid arthritis. Its mechanism offers insights into bradykinin-mediated pathways and potential therapeutic interventions in inflammatory conditions.

    Out of stock

    All 3 sizes
  • B4148
    Cat. No.
    A59147

    B4148

    B4148 is a selective competitive antagonist of the bradykinin receptor, effectively blocking the action of bradykinin. This compound has been shown to significantly inhibit bradykinin-induced hypotension in rat models, particularly in the context of endotoxin shock induced by Escherichia coli lipopolysaccharide. Researchers can utilize B4148 to study vascular responses and blood pressure regulation under inflammatory conditions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • [Des-Arg10]-HOE I40
    Cat. No.
    A59149

    [Des-Arg10]-HOE I40

    [Des-Arg10]-HOE I40 is a potent antagonist of the bradykinin B1 receptor, known for its ability to inhibit bradykinin-induced signaling. This compound plays a significant role in research investigating inflammatory processes and pain pathways, particularly in conditions associated with bradykinin receptor activation. Its effectiveness in blocking B1 receptor activity makes it a valuable tool for studying the therapeutic potential in various pathological states.

    Out of stock

    All 3 sizes
  • Bradykinin B1 receptor antagonist 1
    Cat. No.
    A59153

    Bradykinin B1 receptor antagonist 1

    Bradykinin B1 receptor antagonist 1 is a selective antagonist of the bradykinin B1 receptor, notable for its ability to cross the blood-brain barrier. This compound exhibits efficacy in modulating pain pathways, making it a valuable tool for research into pain mechanisms and potential therapeutic interventions. Its unique action on the bradykinin B1 receptor complements studies focusing on inflammatory responses and pain management.

    25 mg
    $1,405.00
    50 mg
    $1,790.00
    All 3 sizes
  • NPC 17731
    Cat. No.
    A59157

    NPC 17731

    NPC 17731 is a potent bradykinin (BK) receptor antagonist that effectively inhibits both contractile and relaxant responses induced by bradykinin. With an IC50 of 23 nM for contractile effects and 29 nM for relaxant effects, this compound serves as a valuable tool for studying bradykinin signaling pathways. Research applications include investigating cardiovascular responses and potential therapeutic strategies for conditions associated with bradykinin dysregulation.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • FR173657
    Cat. No.
    A59161

    FR173657

    Synonyms: FK-3657

    FR173657 is a potent orally active antagonist of the bradykinin B2 receptor, exhibiting IC50 values of 0.56, 1.5, and 2.9 nM for pig, rat, and human receptors, respectively. This compound effectively inhibits bradykinin-induced bronchoconstriction in guinea pigs with an ED50 of 0.075 mg/kg and demonstrates the ability to reduce carrageenan-induced paw edema in mice at an ED50 of 6.8 mg/kg. FR173657 is valuable for research into inflammatory diseases and related physiological responses.

    25 mg
    $1,780.00
    50 mg
    $2,280.00
    All 3 sizes
  • NPC-567
    Cat. No.
    A59163

    NPC-567

    NPC-567 is a potent bradykinin B2 receptor antagonist. This compound effectively inhibits the acute response to allergens in the airways, making it valuable for research in allergy and respiratory conditions. Its mechanism of action provides a useful tool for exploring the role of bradykinin signaling in inflammatory responses.

    25 mg
    $1,275.00
    All 1 sizes
  • WIN 64338 hydrochloride
    Cat. No.
    A59168

    WIN 64338 hydrochloride

    WIN 64338 hydrochloride is a selective, nonpeptide competitive antagonist of the bradykinin B2 receptor, effectively inhibiting [3H]-Bradykinin binding in human IMR-90 cells with a Ki value of 64 nM. Additionally, this compound demonstrates inhibitory effects on [3H]Quinuclidinyl benzilate binding to rat brain muscarinic receptors, with a Ki of 350 nM. Its ability to modulate bradykinin signaling positions WIN 64338 hydrochloride as a valuable tool for research in pain, inflammation, and cardiovascular studies.

    Out of stock

    All 3 sizes
  • BKM-570
    Cat. No.
    A59169

    BKM-570

    BKM-570 is a nonpeptide bradykinin antagonist that exhibits significant anticancer properties. This compound is valuable for research applications focusing on lung, prostate, and ovarian cancers, providing insights into the role of bradykinin signaling in tumor biology and potential therapeutic approaches. Its antagonistic action contributes to the understanding of bradykinin's involvement in cancer progression.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

22 Items

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