L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
- Product Name
- L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
- CAS No.
- 2411440-41-8
- Chemical Name
- L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
- Synonyms
- JR14a;JR14a ，E1048;JR14a, 10 mM in DMSO;(5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-L-arginine;L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-;inflammation,Inhibitor,inhibit,C3a,JR-14a,Complement System,JR14a,complement;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
- CBNumber
- CB69270798
- Molecular Formula
- C25H26Cl2N4O3S
- Formula Weight
- 533.47
- MOL File
- 2411440-41-8.mol
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Property
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- form
- Solid
- pka
- 3.55±0.21(Predicted)
- color
- White to off-white
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Chemical Properties,Usage,Production
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.
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Suppliers
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