Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC50=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC50=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research.

Product information

CAS Number: 1957278-93-1

Molecular Weight: 406.43

Formula: C20H24F2N4O3

Chemical Name: (5S)-5-cyclopropyl-5-[3-[(3S)-4-(3, 5-difluorophenyl)-3-methylpiperazin-1-yl]-3-oxopropyl]imidazolidine-2, 4-dione

Smiles: C[C@H]1CN(CCN1C1C=C(F)C=C(F)C=1)C(=O)CC[C@]1(NC(=O)NC1=O)C1CC1

InChiKey: CMLVKUWQFZQPPS-YUNKPMOVSA-N

InChi: InChI=1S/C20H24F2N4O3/c1-12-11-25(6-7-26(12)16-9-14(21)8-15(22)10-16)17(27)4-5-20(13-2-3-13)18(28)23-19(29)24-20/h8-10,12-13H,2-7,11H2,1H3,(H2,23,24,28,29)/t12-,20-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (246.04 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 Vivo:

GLPG1972 (oral gavage; 5 mg/kg; single dose) displays a favorable PK profile in mice, rats, and dogs. The oral availability (F%) for mice, rats, and dogs are 25%, 58% and 97%, respectively.

Products are for research use only. Not for human use.