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.
Product information
CAS Number: 2411440-41-8
Molecular Weight: 533.47
Formula: C25H26Cl2N4O3S
Chemical Name: (2S)-2-({5-[bis(4-chlorophenyl)methyl]-3-methylthiophen-2-yl}formamido)-5-[(diaminomethylidene)amino]pentanoic acid
Smiles: CC1C=C(SC=1C(=O)N[C@@H](CCCN=C(N)N)C(O)=O)C(C1C=CC(Cl)=CC=1)C1C=CC(Cl)=CC=1
InChiKey: OHRIKWUZKGNQKQ-IBGZPJMESA-N
InChi: InChI=1S/C25H26Cl2N4O3S/c1-14-13-20(21(15-4-8-17(26)9-5-15)16-6-10-18(27)11-7-16)35-22(14)23(32)31-19(24(33)34)3-2-12-30-25(28)29/h4-11,13,19,21H,2-3,12H2,1H3,(H,31,32)(H,33,34)(H4,28,29,30)/t19-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. JR14a (0.1 nM-100 μM) is metabolically stable to exposure over 1 h to rat liver microsomes. JR14a (0.1 nM-100 μM) inhibits C3a-induced β-hexosaminidase secretion in human LAD2 mast cells, with an IC50 of 8 nM.
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. 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. JR14a (10 mg/kg; p.o.) exhibits Cmax (88 ng/mL), Tmax (300 min) and AUC (478 ng•h/mL) in rats.
Products are for research use only. Not for human use.
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