bradykinin receptor

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Anatibant 2HCl is a small molecule bradykinin B2 receptor antagonist for the treatment of neurological disorders and may be used in the study of brain injury.

Lys-Bradykinin acetate is an endogenous bradykinin receptor agonist.

R715 TFA(185052-09-9 free base) is a potent and selective bradykinin B1 receptor antagonist (pA2 = 8.49). Displays no activity at B2 receptors. Reduces mechanical hypernociception in a mouse model of neuropathic pain. Metabolically stable.

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate ([D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate (96736-12-8 free base)) is a broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.

MK-0686 is an orally available bradykinin B1 receptor antagonist with potential anti-inflammatory activity.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Bombinakinin M acetate is a potent bradykinin receptor agonist with high selectivity for mammalian arterial smooth muscle bradykinin receptors and is approximately 50 times more potent than bradykinin.

Lys-[Des-Arg9]Bradykinin,TFA is Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

(Hyp³)-Bradykinin acetate is an agonist of bradykinin B2 receptor and stimulates inositol phosphate production in cultured human fibroblasts.

[Des-Arg9]-Bradykinin is an agonist of Bradykinin (B1) receptor that displays selectivity for B1 over B2 receptors.

Anatibant is a potent non-peptide bradykinin B2 receptor antagonist. Anatibant reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury.

Icatibant is a selective and specific antagonist of the bradykinin B2 receptor (IC50 and Ki: 1.07 nM and 0.798 nM respectively).

Bradykinin is an inflammatory mediator. It is a peptide that causes blood vessels to dilate (enlarge) via the release of prostacyclin, nitric oxide, and Endothelium-Derived Hyperpolarizing Factor. Bradykinin is a physiologically and pharmacologically active peptide of the kinin group of proteins, consisting of nine amino acids.

Bradykinin (2-9) (Des-Arg1-bradykinin) is an amino-truncated peptide compound that is a metabolite of Bradykinin. It is formed by the cleavage action of Aminopeptidase P.

[Des-Arg9]-Bradykinin acetate is a selective agonist of the Bradykinin B1 receptor.

ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors.

FR190997 is an agonist of bradykinin B2 receptor.

Labradimil is a bradykinin B2 receptor agonist. Labradimil increases the permeability of human brain microvascular endothelial cell monolayers. Labradimil enhances delivery of hydrophilic chemotherapeutics and increases survival in rats with metastatic tu

The chimeric peptide M35 [galanin (1-13)-bradykinin(2-9) amide] is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. The radiolabelled M35 and perf

Potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

Selective bradykinin B2 receptor agonist that is resistant to carboxypeptidase cleavage. 5-fold more potent and exhibits a more prolonged duration of action than bradykinin in vivo.

NVP-SAA164 is a nonpeptide bradykinin B1 receptor antagonist agent.

Icatibant Acetate, an antagonist of the bradykinin B2 receptor, is used in the treatment of hereditary angioedema.

Fulimetibant is a bradykinin receptor antagonist.

Potent and selective bradykinin B1 receptor antagonist (ID50 values are 2.8 and > 600 nM at B1 and B2 receptors respectively). Exhibits no intrinsic agonist activity and is resistant to aminopeptidase and kininase II (ACE) cleavage. Displays hypertensive

Deltibantis a bradykinin receptor antagonist.

SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).

Lys-(Des-Arg9,Leu8)-Bradykinin is a selective antagonist of the bradykinin B1 receptor [1].

Potent bradykinin receptor agonist. Highly selective for mammalian arterial smooth muscle bradykinin receptors, displaying ~ 50-fold greater potency than bradykinin. Elicits dose-dependent contractile effects in smooth muscle of guinea pig ileum (EC50 = 4

Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]

NPC 17761 is a bradykinin receptor antagonist.

NPC 17731 is a bradykinin receptor antagonist.

FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.

Lys-[Des-Arg9]Bradykinin TFA is a naturally occurring kinin that serves as a potent and highly selective agonist for the bradykinin B1 receptor, demonstrating binding affinities (K i values) of 0.12 nM, 1.7 nM, and 0.23 nM for the human, mouse, and rabbit B1 receptors, respectively. This compound exhibits low inhibitory activity on B2 receptors [1] [2].

Endogenous bradykinin receptor agonist

Peptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140. Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).

Des-Arg9-[Leu8]-Bradykinin acetate is a potent antagonist of the bradykinin receptor 1 (B1R) used in renal fibrosis research [1].

NPC 567 is an antagonist of the bradykinin receptor.

Deucrictibant is a bradykinin receptor antagonist.

R 715, a bradykinin B1 receptor antagonist, inhibits contractions in isolated human umbilical cords that express bradykinin B1 receptors (pA2 = 8.49). When administered at doses of 200, 400, and 600 µg/kg, R 715 enhances latency to tail withdrawal in the tail-flick test for diabetic neuropathy mouse models induced by streptozotocin (STZ), signaling potential analgesic properties. Furthermore, at a 1 mg/kg per day dosage, it mitigates symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE) induced by MOG35-55 antigen peptide, such as reducing hind limb weakness and paralysis, improving gait symmetry, and decreasing spinal inflammation, neuron demyelination, and lesion monocyte invasion. Additionally, R 715 at 0.01 nmol/animal, administered intracerebroventricularly (i.c.v.), lowers mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats, indicating cardiovascular effects.

B 9430 is a potent bradykinin B1 B2 receptor antagonist [1].

[Tyr8] Bradykinin, a B2 kinin receptor agonist, not only stimulates ERK1/2 phosphorylation but also serves as an internal standard [1].

JMV-1645 is an effective and selective B(1) bradykinin receptor antagonist.

Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. In

[Des-Arg10]-HOE 140 is a bioactive peptide that functions as a potent B1 bradykinin receptor antagonist.

[Des-Arg9]-Bradykinin ([Des-Arg9]-Bradykinin(2TFA))(2TFA) is an agonist of Bradykinin (B1) receptor.

FK-3657 is a non-peptide antagonist of bradykinin (BK)-B2 receptor.

Bradykinin (1-7), an amino-truncated peptide derived from Bradykinin, is a metabolite formed through enzymatic cleavage by endopeptidase.

Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE). The Bradykinin (BK) fragment (1-5) (RPPGF) is one of the most stable naturally occurring metabolites and may be used as a marker for BK production in vivo.

Bradykinin (1-6) is an amino-truncated Bradykinin peptide and a stable metabolite of Bradykinin, cleaved by carboxypeptidase Y (CPY). This fragment of Bradykinin activates pain receptors and induces smooth muscle contraction.

Bradykinin (1-3) is a fragment of Bradykinin, which activates pain receptors.

Bradykinin (acetate) 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. Enzymatically produced from kallidin in the blood, it is a powerful vasodilator that causes smooth muscle contraction, and may mediate inflammation. It has a role as a human blood serum metabolite and a vasodilator agent. It is a tautomer of a bradykinin(2+).