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GB83
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C32H44N4O4
- MW: 548.72
Description
GB83 is a selective human protease activated receptor 2 (PAR2) antagonist with an IC50 value of 2 μM. GB83 reversibly inhibits PAR2 activation by both proteases and other PAR2 agonists.
PAR2 is a G protein-coupled receptor activated by proteolytic cleavage and involved in inflammation, pain signaling, vascular responses, epithelial barrier regulation, and immune cell activation. GB83 is a useful pharmacological tool for studying PAR2-mediated signaling and protease-dependent receptor activation.
Key Features
- Selective human PAR2 antagonist
- IC50: 2 μM
- Reversibly inhibits PAR2 activation
- Blocks activation by proteases and PAR2 agonists
- Useful tool for protease receptor signaling research
Applications
- PAR2 receptor pharmacology
- Protease activated receptor signaling studies
- Inflammation and pain pathway research
- GPCR activation and signaling investigations
- Protease-mediated cellular response studies
More Information
| Parent CAS No. | 1252806-86-2 |
|---|---|
| Chemical Name | N-((S)-3-cyclohexyl-1-((2S,3S)-1-(2,3-dihydrospiro[indene-1,4'-piperidine]-1'-yl)-3-methyl-1-oxopentan-2-ylamino)-1-oxopropan-2-yl)isoxazole-5-carboxamide |
| SMILES | C1=C(C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(N2CCC3(CCC4C=CC=CC3=4)CC2)=O)CC2CCCCC2)ON=C1 |&1:5,9,10,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C32H44N4O4/c1-3-22(2)28(31(39)36-19-16-32(17-20-36)15-13-24-11-7-8-12-25(24)32)35-29(37)26(21-23-9-5-4-6-10-23)34-30(38)27-14-18-33-40-27/h7-8,11-12,14,18,22-23,26,28H,3-6,9-10,13,15-17,19-21H2,1-2H3,(H,34,38)(H,35,37)/t22?,26-,28-/m0/s1 |
| InChiKey | ZXMXAOYWSLZLQM-NZNGGYBSSA-N |
| CID | 49843509 |
| Short Description | PAR2 antagonist |
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