GLPG3970 | CAS#2403733-82-2 | first-in-class dual SIK2/SIK3 inhibitor

MedKoo Cat#: 126665 | Name: GLPG3970

Description:

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

GLPG3970 is a first-in-class dual SIK2/SIK3 inhibitor with selectivity against SIK1 (IC50 of 282.8 nM on SIK1, 7.8 nM on SIK2 and 3.8 nM on SIK3). The dual activity of GLPG3970 in modulating the pro-inflammatory cytokine TNFα and the immunoregulatory cytokine IL-10 is demonstrated in vitro in human primary myeloid cells and human whole blood, and in vivo in mice stimulated with lipopolysaccharide. GLPG3970 shows dose-dependent activity in disease-relevant mouse pharmacological models.

Chemical Structure

GLPG3970

CAS#2403733-82-2

Theoretical Analysis

MedKoo Cat#: 126665

Name: GLPG3970

CAS#: 2403733-82-2

Chemical Formula: C25H27F3N4O4

Exact Mass: 504.1984

Molecular Weight: 504.51

Elemental Analysis: C, 59.52; H, 5.39; F, 11.30; N, 11.11; O, 12.68

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

GLPG3970; GLPG-3970; GLPG 3970

IUPAC/Chemical Name

8-methoxy-6-(7-(2-morpholinoethoxy)imidazo[1,2-a]pyridin-3-yl)-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1(2H)-one

InChi Key

XASOHFCUIQARJT-UHFFFAOYSA-N

InChi Code

InChI=1S/C25H27F3N4O4/c1-34-21-13-18(12-17-2-4-31(16-25(26,27)28)24(33)23(17)21)20-15-29-22-14-19(3-5-32(20)22)36-11-8-30-6-9-35-10-7-30/h3,5,12-15H,2,4,6-11,16H2,1H3

SMILES Code

COC1=CC(C2=CN=C3N2C=CC(OCCN4CCOCC4)=C3)=CC5=C1C(N(CC(F)(F)F)CC5)=O

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 504.51 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.

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

1: Peixoto C, Joncour A, Temal-Laib T, Tirera A, Dos Santos A, Jary H, Bucher D, Laenen W, Pereira Fernandes A, Lavazais S, Delachaume C, Merciris D, Saccomani C, Drennan M, López-Ramos M, Wakselman E, Dupont S, Borgonovi M, Roca Magadan C, Monjardet A, Brys R, De Vos S, Andrews M, Jimenez JM, Amantini D, Desroy N. Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases. J Med Chem. 2024 Mar 29. doi: 10.1021/acs.jmedchem.3c02246. Epub ahead of print. PMID: 38552030. 2: Zhu W, Liu X, Li Q, Gao F, Liu T, Chen X, Zhang M, Aliper A, Ren F, Ding X, Zhavoronkov A. Discovery of novel and selective SIK2 inhibitors by the application of AlphaFold structures and generative models. Bioorg Med Chem. 2023 Aug 15;91:117414. doi: 10.1016/j.bmc.2023.117414. Epub 2023 Jul 13. PMID: 37467565.