A non-peptide antagonist of C3aR

SB 290157 (trifluoroacetate salt) – 10 mg

Brand:
Cayman
CAS:
1140525-25-2
Storage:
-20
UN-No:
Non-Hazardous - /

The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}  

 

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Description

A non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM; potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM); also effective in vivo, reducing inflammation in a variety of animal models

Formal name: N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate

Synonyms: 

Molecular weight: 526.5

CAS: 1140525-25-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Immunology & Inflammation|Innate Immunity

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