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C3aR antagonist JR14a

Chemical Structure : C3aR antagonist JR14a

CAS No.: 2411440-41-8

C3aR antagonist JR14a (JR14a)

Catalog No.: PC-72006Not For Human Use, Lab Use Only.

C3aR antagonist JR14a is a potent and selective antagonist of human Complement C3a receptor (hC3aR) with IC50 of 10 nM (Inhibition of intracellular Ca2+ release induced by 100 nM C3a).

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Biological Activity

C3aR antagonist JR14a is a potent and selective antagonist of human Complement C3a receptor (hC3aR) with IC50 of 10 nM (Inhibition of intracellular Ca2+ release induced by 100 nM C3a).
JR14a shows no agonist activity against hC3aR and 100-fold more potent than SB290157 (Cat. PC-60789).
JR14a inhibited β-hexosaminidase secretion (IC50=8 nM) from human LAD2 mast cells degranulated by 100 nM C3a.
JR14a demonstarted anti-inflammatory activity against agonist-induced paw edema in male Wistar rats.

Physicochemical Properties

M.Wt 533.468
Formula C25H26Cl2N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5-(bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-L-arginine

References

1. Jessica A Rowley, et al. J Med Chem. 2020 Jan 23;63(2):529-541.

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