Description
GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
Product information
CAS Number: 1252806-70-4
Molecular Weight: 608.77
Formula: C33H48N6O5
Chemical Name: (2S,3S)-N-({3-[4-(aminomethyl)piperidine-1-carbonyl]phenyl}methyl)-2-[(2S)-3-cyclohexyl-2-[(1,2-oxazol-5-yl)formamido]propanamido]-3-methylpentanamide
Smiles: C[C@@H](CC)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=CC=NO1)C(=O)NCC1C=C(C=CC=1)C(=O)N1CCC(CN)CC1
InChiKey: HXLQLJFWNKMGET-NVLPUFGLSA-N
InChi: InChI=1S/C33H48N6O5/c1-3-22(2)29(38-30(40)27(19-23-8-5-4-6-9-23)37-31(41)28-12-15-36-44-28)32(42)35-21-25-10-7-11-26(18-25)33(43)39-16-13-24(20-34)14-17-39/h7,10-12,15,18,22-24,27,29H,3-6,8-9,13-14,16-17,19-21,34H2,1-2H3,(H,35,42)(H,37,41)(H,38,40)/t22-,27-,29-/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:
In an intracellular Ca2+ (iCa2+) mobilization assay using HT29 colon cancer cells, GB110 (EC50 240±20 nM; pEC50 6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC50 210±30 nM; pEC50 6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC50 6±0.5 nM; pEC50 8.2±0.8).
References:
- Barry GD, et al. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40.
- Suen JY, et al. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.