GLPG0259 A | CAS# 1195065-29-2 | MAPKAPK5 inhibitor

MedKoo Cat#: 555814 | Name: GLPG0259 A

Description:

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

GLPG0259 A is a small-molecule inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5), a kinase enzyme that plays a role in important inflammatory pathways.

Chemical Structure

GLPG0259 A

CAS# 1195065-29-2 (GLPG0259 A)

Theoretical Analysis

MedKoo Cat#: 555814

Name: GLPG0259 A

CAS#: 1195065-29-2 (GLPG0259 A)

Chemical Formula: C24H26N8O2

Exact Mass: 458.2179

Molecular Weight: 458.53

Elemental Analysis: C, 62.87; H, 5.72; N, 24.44; O, 6.98

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.

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Related CAS #

1195065-29-2 (GLPG0259 A) 959754-85-9

Synonym

GLPG-0259 A; GLPG 0259 A; GLPG0259 A; GLPG-0259A; GLPG 0259A; GLPG0259A;

IUPAC/Chemical Name

4-[8-({4-[(1S,4S)-5-(propan-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]phenyl}amino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl]furan-2-carboxamide

InChi Key

YBFGSJUVEOYPIS-OALUTQOASA-N

InChi Code

InChI=1S/C24H26N8O2/c1-14(2)30-10-19-8-18(30)11-31(19)17-5-3-16(4-6-17)29-23-24-27-13-28-32(24)20(9-26-23)15-7-21(22(25)33)34-12-15/h3-7,9,12-14,18-19H,8,10-11H2,1-2H3,(H2,25,33)(H,26,29)/t18-,19-/m0/s1

SMILES Code

O=C(C1=CC(C2=CN=C(NC3=CC=C(N4[C@](C5)([H])CN(C(C)C)[C@]5([H])C4)C=C3)C6=NC=NN62)=CO1)N

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 458.53 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: Westhovens R, Keyser FD, Rekalov D, Nasonov EL, Beetens J, Van der Aa A, Wigerinck P, Namour F, Vanhoutte F, Durez P. Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial. Ann Rheum Dis. 2013 May;72(5):741-4. doi: 10.1136/annrheumdis-2012-202221. Epub 2012 Nov 17. PubMed PMID: 23161899. 2: Namour F, Vanhoutte FP, Beetens J, Blockhuys S, De Weer M, Wigerinck P. Pharmacokinetics, safety, and tolerability of GLPG0259, a mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5) inhibitor, given as single and multiple doses to healthy male subjects. Drugs R D. 2012 Sep 1;12(3):141-63. doi: 10.2165/11633120-000000000-00000. PubMed PMID: 22950522; PubMed Central PMCID: PMC3585965.