Description
GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM.
Product information
CAS Number: 1416435-96-5
Molecular Weight: 546.70
Formula: C32H42N4O4
Chemical Name: (2S)-3-cyclohexyl-N-[(2S,3S)-3-methyl-1-oxo-1-{spiro[indene-1,4'-piperidin]-1'-yl}pentan-2-yl]-2-[(1,2-oxazol-5-yl)formamido]propanamide
Smiles: C[C@@H](CC)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=CC=NO1)C(=O)N1CCC2(CC1)C=CC1=CC=CC=C21
InChiKey: DCUDDCGUKZLQLN-MCOVPRHSSA-N
InChi: InChI=1S/C32H42N4O4/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/h7-8,11-15,18,22-23,26,28H,3-6,9-10,16-17,19-21H2,1-2H3,(H,34,38)(H,35,37)/t22-,26-,28-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 31.25 mg/mL (57.16 mM; Need ultrasonic).
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:
GB-88 inhibits iCa2+ release induced in HT29 cells by trypsin, 2f-LIGRLO-NH2 and GB110 (PAR2 agonists). And antagonism by GB-88 is agonist dependent.
In Vivo:
GB-88 (10 mg/kg, p.o. in olive oil) is both orally active and anti-inflammatory in vivo, with specific antagonist activity against four structurally and mechanistically different PAR2 agonists (2f-LIGRLO-NH2, trypsin, SLIGRL-NH2 and GB110). GB-88 inhibits PAR2-induced acute inflammation in vivo.
Products are for research use only. Not for human use.
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