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BR103

MCE China：BR103

Brand：MedChemExpress (MCE)

Cat. No.HY-117992

CAS：1434873-26-3

Purity：99.75%

Storage：-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding.

In Vivo：BR103 can be used in animal modeling to create inflammatory paw edema models in Wistar rats. BR103 remains structurally intact and undegraded after in vitro exposure to rat plasma and rat liver microsomes, which are rich in cytochrome P450 enzymes. This in vitro stability of BR103 suggests potentially low in vivo clearance, high stability, and bioavailability. Paw edema induced by subplantar injection of BR103 peaks at 0.5 hours and resolves by 24 hours[2][3]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of inflammatory paw edema[2][3] Background BR103 selectively activates Complement C3a receptor (C3aR), leading to mast cell activation and thereby inducing acute inflammatory edema and immune response[2][3]. Specific Mmodeling Methods Rat: Wistar • male • 8-week-oldAdministration: 350 ng • Intraplantar (i.pl.) injection • single dose Note 350 μg BR103 is dissolved in 100 μL of 5% DMSO or isotonic saline. Modeling Indicators Molecular changes: Activation of mast cells, macrophages, and neutrophils, as well as myeloperoxidase (MPO); release of histamine and tryptase; increased and recruited leukocytes at the administration site; upregulation of pro-inflammatory factors (Il1β, Il6, Tnf, Ccl3, and Mcp1).Histological changes: Localized paw edema; infiltration of macrophages and neutrophils at the inflammation site. Correlated Product(s): λ-Carrageenan (HY-N9470) Opposite Product(s): /

IC50 & Target：C3aR[1] In Vivo BR103 can be used in animal modeling to create inflammatory paw edema models in Wistar rats. BR103 remains structurally intact and undegraded after in vitro exposure to rat plasma and rat liver microsomes, which are rich in cytochrome P450 enzymes. This in vitro stability of BR103 suggests potentially low in vivo clearance, high stability, and bioavailability. Paw edema induced by subplantar injection of BR103 peaks at 0.5 hours and resolves by 24 hours[2][3]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of inflammatory paw edema[2][3] Background BR103 selectively activates Complement C3a receptor (C3aR), leading to mast cell activation and thereby inducing acute inflammatory edema and immune response[2][3]. Specific Mmodeling Methods Rat: Wistar • male • 8-week-oldAdministration: 350 ng • Intraplantar (i.pl.) injection • single dose Note 350 μg BR103 is dissolved in 100 μL of 5% DMSO or isotonic saline. Modeling Indicators Molecular changes: Activation of mast cells, macrophages, and neutrophils, as well as myeloperoxidase (MPO); release of histamine and tryptase; increased and recruited leukocytes at the administration site; upregulation of pro-inflammatory factors (Il1β, Il6, Tnf, Ccl3, and Mcp1).Histological changes: Localized paw edema; infiltration of macrophages and neutrophils at the inflammation site. Correlated Product(s): λ-Carrageenan (HY-N9470) Opposite Product(s): / MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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References：

[1]. Dantas de Araujo A, et al. Europium-Labeled Synthetic C3a Protein as a Novel Fluorescent Probe for Human Complement C3a Receptor. Bioconjug Chem. 2017 Jun 21;28(6):1669-1676.  [Content Brief]

[2]. Lohman RJ, et al. Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Nat Commun. 2017 Aug 24;8(1):351.  [Content Brief]

[3]. Rowley JA, et al. Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. J Med Chem. 2020 Jan 23;63(2):529-541.  [Content Brief]