Bradykinin receptors are G protein-coupled receptors (GPCRs), which are found on the surface of cells. B1 and B2 are the two subtypes of bradykinin receptors. Bradykinin receptor-mediated signal transductions are important for regulating pain and inflammation as well as maintaining cardiovascular homeostasis. Both receptors activate G-proteins to transmit extracellular signals.
Bradykinin B2 receptor is ubiquitous and is expressed constitutively, whereas bradykinin B1 receptor is expressed at a very low level in healthy tissues but is induced under stressful conditions like shock or inflammation. Vasodilation, osmoregulation, smooth muscle contraction, and nociceptor activation are all regulated by the bradykinin B2 receptor. Since the bradykinin B1 receptor and bradykinin B2 receptor are linked to inflammatory disease, vasculopathy, neuropathy, obesity, diabetes, and cancer, they have become potential therapeutic targets. B1R and B2R may play opposing roles in various diseases. Therapeutic evaluations of antagonists and agonists have been conducted.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V75325 | [Phe8Ψ(CH-NH)Arg9]-Bradykinin | 118122-39-7 | [Phe8Ψ(CH-NH)Arg9]-Bradykinin is a selective bradykinin B2 receptor agonist (activator) (not cleaved by protein kinase I/II). |
|
V75328 | B 9430 | 180981-09-3 | B 9430 is a potent bradykinin B1/B2 receptor blocker (antagonist). |
|
V75318 | BA 1 | 183241-31-8 | BA 1 is a bombesin (BB) receptor family agonist. |
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V75319 | BIM-26226 | 136207-23-3 | BIM-26226 is a gastrin-releasing peptide and a potent and specific bombesin receptor antagonist. |
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V75323 | Bombinakinin M | 509151-65-9 | Bombinakinin M is a bradykinin receptor agonist (activator) with contractile activity in the guinea pig ileum. |
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V75317 | BRS-3 receptor agonist-2 | 1021937-07-4 | BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist/activator with EC50 of 2.5 nM for mouse BRS-3 receptor. |
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V75324 | Des-Arg9-[Leu8]-Bradykinin acetate | 115035-45-5 | Des-Arg9-[Leu8]-Bradykinin acetate is a potent bradykinin receptor 1 (B1R) antagonist. |
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V20458 | ELN441958 | 913064-47-8 | ELN441958 (ELN-441958) is a novel, potent, and small molecule antagonist of neutral bradykinin B1 receptor which inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. |
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V75322 | Fasitibant chloride (MEN16132 free base) | 1157852-02-2 | Fasitibant chloride (MEN16132 free base) is a specific, non-peptide bradykinin B2 receptor (B2R) antagonist. |
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V75330 | Fasitibant free base | 869939-83-3 | Fasitibant (free base) is a specific, high-affinity, long-acting non-peptide bradykinin B2 receptor (BK2 receptor) antagonist. |
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V75316 | GB-6 | 2413262-74-3 | GB-6 is a short linear peptide that targets the gastrin-releasing peptide receptor (GRPR). |
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V20875 | Icatibant | 130308-48-4 | Icatibant (HOE-140) is a potent and specific bradykinin B2 receptor blocker (antagonist) with IC50 and Kis of 1.07 nM and 0.798 nM respectively. |
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V75331 | Icatibant acetate (HOE 140 acetate) | 138614-30-9 | Icatibant acetate (HOE-140 acetate) is a potent and specific bradykinin B2 receptor antagonist (inhibitor) with IC50 and Kis of 1.07 nM and 0.798 nM respectively. |
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V75329 | Lys-[Des-Arg9]Bradykinin TFA | 2763588-90-3 | Lys-[Des-Arg9]Bradykinin TFA is a naturally occurring kinin that is a potent and selective bradykinin B1 receptor agonist/activator with Kis for B1 receptors in humans, mice and rabbits. |
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V75327 | Lys-[Hyp3]-Bradykinin | 113662-39-8 | Lys-[Hyp3]-Bradykinin is an agonist of Bradykinin. |
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V75321 | MEN 11270 | 235082-52-7 | MEN 11270 is a cyclic decapeptide and a B2 kinin receptor antagonist. |
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V75326 | R715 | 185052-09-9 | R715 is a selective bradykinin B1 receptor blocker (antagonist). |
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V75320 | Sar-[D-Phe8]-des-Arg9-Bradykinin | 126959-88-4 | Sar-[D-Phe8]-des-Arg9-Bradykinin is a B1 receptor agonist. |
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V3106 | SSR-240612 HCl | 464930-42-5 | SSR-240612 HCl, the hydrochloride salt of SSR240612, is a novel, potent, and orally bioactive specific non-peptide bradykinin B(1) receptor antagonist. |
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