1. Immunology/Inflammation
  2. Complement System
  3. JR14a

JR14a 

Cat. No.: HY-138161
Handling Instructions

JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation.

For research use only. We do not sell to patients.

JR14a Chemical Structure

JR14a Chemical Structure

CAS No. : 2411440-41-8

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Description

JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation[1].

IC50 & Target

human complement C3a receptor[1]

In Vitro

JR14a (0.1 nM-100 μM) inhibits C3a-induced intracellular Ca2+ release in human monocyte-derived macrophages, with an IC50 of 10 nM[1].
JR14a (0.1 nM-100 μM) is metabolically stable to exposure over 1 h to rat liver microsomes[1].
JR14a (0.1 nM-100 μM) inhibits C3a-induced β-hexosaminidase secretion in human LAD2 mast cells, with an IC50 of 8 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JR14a (10 mg/kg; p.o. 2 h prior) reduces paw swelling by 65% over control at 30 min after agonist injection in acute rat paw model of inflammation and edema[1].
JR14a (1 mg/kg; i.v.) exhibits elimination half-life (191 min), clearance (4.4 mL/min/kg) and AUC (3795 ng•h/mL) in rats[1].
JR14a (10 mg/kg; p.o.) exhibits Cmax (88 ng/mL), Tmax (300 min) and AUC (478 ng•h/mL) in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wister rats (8 weeks, 250-300 g) were injected with BR103[1]
Dosage: 10 mg/kg
Administration: P.o. 2 h prior to agonist challenge
Result: Inhibited C3aR-mediated inflammation.
Animal Model: Male Wister rats (8 weeks, 250-300 g)[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: t1/2=191 min, clearance=4.4 mL/min/kg, AUC=3795 ng•h/mL.
P.o.: Cmax=88 ng/mL, Tmax=300 min, AUC=478 ng•h/mL.
Molecular Weight

533.47

Formula

C₂₅H₂₆Cl₂N₄O₃S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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JR14a
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