| Identification | Back Directory | [Name]
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- | [CAS]
2411440-41-8 | [Synonyms]
JR14a
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-l-arginine hydrochloride
(S)-2-(5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carboxamido)-5-guanidinopentanoic acid | [Molecular Formula]
C25H26Cl2N4O3S | [MDL Number]
MFCD34471093 | [MOL File]
2411440-41-8.mol | [Molecular Weight]
533.47 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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].
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]. | [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]. | 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.
|
| [References]
[1]. 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. |
|
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|