This product is a potent C5a receptor antagonist, it inhibits C3aR with the IC50 of 20 nM. It is also a MrgX2 agonist and inhibits C5a-induced hypernociception in rats.
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CAS No. | 219639-75-5 |
Formula | C47H65N11O7 |
Molecular Weight | 896.1 |
Sequence | FXPXWR (Modifications: Phe-1 = N-terminal Ac, X-2 = Orn, X-4 = D-Cha, Lactam bridge: Orn-2 to Arg-6 ) |
SMILES | NC(=NCCCC1NC(=O)C(NC(=O)C(CC2CCCCC2)NC(=O)C2N(C(=O)C(CCCNC1=O)NC(=O)C(Cc1ccccc1)NC(=O)C)CCC2)Cc1c[nH]c2c1cccc2)N |
IC50 | IC50: 20nM |
Purity | 98% |
Solubility | H2O: 2 mg/ml |
Storage | Store at -20°C for short term; at -80 °C for long-term storage. |
Target | C5a |
Introduction | Complement component C5a, a type of anaphylatoxins, is one of the most potent effectors generated via cleavage of C5 molecule during complement activation. C5a binds two receptors, C5aR and C5L2. Most of the C5a functional effects occur by binding to C5aRs, a G-protein-coupled signaling receptor that has long been identified as an attractive drug target. |