MedKoo Cat#: 573468 | Name: AGG-523
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury.

Chemical Structure

AGG-523
AGG-523
CAS#920289-29-8

Theoretical Analysis

MedKoo Cat#: 573468

Name: AGG-523

CAS#: 920289-29-8

Chemical Formula: C28H29FN2O4

Exact Mass: 476.2111

Molecular Weight: 476.55

Elemental Analysis: C, 70.57; H, 6.13; F, 3.99; N, 5.88; O, 13.43

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to Ship
5mg USD 350.00 Ready to Ship
10mg USD 550.00 Ready to Ship
25mg USD 950.00 Ready to Ship
50mg USD 1,650.00 Ready to Ship
100mg USD 2,950.00 Ready to Ship
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Related CAS #
No Data
Synonym
AGG-523; AGG 523; AGG523; PF-05212371; PF 05212371; PF05212371; WAY-266523; WAY 266523; WAY266523;
IUPAC/Chemical Name
Pentanoic acid, 4-(((1,1'-biphenyl)-4-ylcarbonyl)amino)-5-((2-(4-fluorophenyl)-1,1-dimethylethyl)amino)-5-oxo-, (4S)-
InChi Key
JWQMTWCFNZSLNR-DEOSSOPVSA-N
InChi Code
1S/C28H29FN2O4/c1-28(2,18-19-8-14-23(29)15-9-19)31-27(35)24(16-17-25(32)33)30-26(34)22-12-10-21(11-13-22)20-6-4-3-5-7-20/h3-15,24H,16-18H2,1-2H3,(H,30,34)(H,31,35)(H,32,33)/t24-/m0/s1
SMILES Code
CC(C)(Cc1ccc(F)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)c2ccc(cc2)c3ccccc3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model.
In vitro activity:
TBD
In vivo activity:
Similarly, synovial fluid ARG-aggrecan levels increased following surgically-induced joint instability in the rat MT model, which was significantly attenuated by orally dosing the animals with AGG-523, an aggrecanase specific inhibitor. Reference: Osteoarthritis Cartilage. 2011 Mar;19(3):315-23. https://pubmed.ncbi.nlm.nih.gov/21163358/

Preparing Stock Solutions

The following data is based on the product molecular weight 476.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chockalingam PS, Sun W, Rivera-Bermudez MA, Zeng W, Dufield DR, Larsson S, Lohmander LS, Flannery CR, Glasson SS, Georgiadis KE, Morris EA. Elevated aggrecanase activity in a rat model of joint injury is attenuated by an aggrecanase specific inhibitor. Osteoarthritis Cartilage. 2011 Mar;19(3):315-23. doi: 10.1016/j.joca.2010.12.004. Epub 2010 Dec 14. PMID: 21163358.
In vitro protocol:
TBD
In vivo protocol:
1. Chockalingam PS, Sun W, Rivera-Bermudez MA, Zeng W, Dufield DR, Larsson S, Lohmander LS, Flannery CR, Glasson SS, Georgiadis KE, Morris EA. Elevated aggrecanase activity in a rat model of joint injury is attenuated by an aggrecanase specific inhibitor. Osteoarthritis Cartilage. 2011 Mar;19(3):315-23. doi: 10.1016/j.joca.2010.12.004. Epub 2010 Dec 14. PMID: 21163358.
1: Chockalingam PS, Sun W, Rivera-Bermudez MA, Zeng W, Dufield DR, Larsson S, Lohmander LS, Flannery CR, Glasson SS, Georgiadis KE, Morris EA. Elevated aggrecanase activity in a rat model of joint injury is attenuated by an aggrecanase specific inhibitor. Osteoarthritis Cartilage. 2011 Mar;19(3):315-23. doi: 10.1016/j.joca.2010.12.004. Epub 2010 Dec 14. PubMed PMID: 21163358.