A competitive antagonist of C5aR (IC50 = 11.6 nM for the human recombinant receptor); has inverse agonist activity; selective for human recombinant over rat and mouse recombinant C5aRs (IC50 = >10 µM for both) but does have activity at macaque and gerbil receptors (IC50s = 7.3 and 6.4 nM

NDT 9513727 – 10 mg

Brand:
Cayman
CAS:
439571-48-9
Storage:
-20
UN-No:
Non-Hazardous - /

NDT 9513727 is a competitive antagonist of the C5a receptor (C5aR; IC50 = 11.6 nM for human recombinant receptors) that has inverse agonist activity in a GTPγ[35S] assay.{35197,43605} It is selective for human recombinant over rat and mouse recombinant C5aRs (IC50 = >10 µM for both) but does have activity at macaque and gerbil receptors (IC50s = 7.3 and 6.4 nM, respectively). NDT 9513727 inhibits degranulation in U937 cells stimulated with C5a (IC50 = 7.1 nM). It also prevents neutropenia induced by human recombinant C5a in gerbils (ED50 = 2.2 mg/kg) and in cynomolgus macaques when administered at doses of 5 and 25 mg/kg.{43605}  

 

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SKU: 24448 - 10 mg Category:

Description

A competitive antagonist of C5aR (IC50 = 11.6 nM for the human recombinant receptor); has inverse agonist activity; selective for human recombinant over rat and mouse recombinant C5aRs (IC50 = >10 µM for both) but does have activity at macaque and gerbil receptors (IC50s = 7.3 and 6.4 nM, respectively); inhibits degranulation in C5a-stimulated U937 cells (IC50 = 7.1 nM); prevents C5a-induced neutropenia in gerbils (ED50 = 2.2 mg/kg) and in cynomolgus macaques at 5 and 25 mg/kg

Formal name: N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine

Synonyms: 

Molecular weight: 573.7

CAS: 439571-48-9

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Innate Immunity

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