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MPMKMQHJHDHPBE-RUZDIDTESA-N

Product Name
MPMKMQHJHDHPBE-RUZDIDTESA-N
CAS No.
1391076-61-1
Chemical Name
MPMKMQHJHDHPBE-RUZDIDTESA-N
Synonyms
GLPG 0974 (GLPG0974);GLPG0974, 10 mM in DMSO;MPMKMQHJHDHPBE-RUZDIDTESA-N;4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid;Butanoic acid, 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-
CBNumber
CB93551520
Molecular Formula
C25H25ClN2O4S
Formula Weight
484.99
MOL File
1391076-61-1.mol
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MPMKMQHJHDHPBE-RUZDIDTESA-N Property

Boiling point:
726.3±60.0 °C(Predicted)
Density 
1.374±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: soluble; Ethanol: soluble
form 
A solid
pka
4.63±0.10(Predicted)
color 
Off-white to light yellow
optical activity
[α]/D +175 to +200°, c =1 in chloroform-d
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2443
Product name
GLPG0974
Purity
≥98% (HPLC)
Packaging
5MG
Price
$159
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2443
Product name
GLPG0974
Purity
≥98% (HPLC)
Packaging
25MG
Price
$633
Updated
2025/07/31
Cayman Chemical
Product number
28108
Product name
GLPG0974
Packaging
1mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
28108
Product name
GLPG0974
Packaging
5mg
Price
$135
Updated
2024/03/01
TRC
Product number
G411803
Product name
GLPG0974
Packaging
2.5mg
Price
$260
Updated
2021/12/16
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MPMKMQHJHDHPBE-RUZDIDTESA-N Chemical Properties,Usage,Production

Uses

GLPG 0974 is a potent FFA2 antagonist.

Biological Activity

GLPG0974 is an orally available, high-affinity, potent and selective free fatty acid receptor 2 (FFA2; FFAR2; GPCR43; GPR43) antagonist (hFFA2 Kd = 7.5 nM; IC50 = 9 nM; Na acetate EC80-induced Ca2+ flux in HEK293 hFFA2 transfectants) with little potency toward 55 other receptors/channels/transporters (IC50 >10 μM), including FFA3 (GPR41). GLPG0974 inhibits acetate-induced human neutrophil migration (IC50 = 27 nM) and exhibits in vivo efficacy (0.1 or 1 mg/kg intragastrically) against duodenal lesions induction by NSAID indomethacin/FFA2 agonist phenylacetamide-1 co-treatment with good pharmacokinetic properties and oral availability (F = 47% in rats; 5 mg/kg p.o.).

in vivo

GLPG0974 shows excellent pharmacokinetic properties in rat with a bioavailability of 47% and a linear increase of the plasma exposure after oral dosing at 5 and 30 mg/kg. The extended half-life observed following the increase of oral dose is consistent with the project objective to obtain long target coverage in human[1].

storage

Store at +4°C

MPMKMQHJHDHPBE-RUZDIDTESA-N Preparation Products And Raw materials

Raw materials

Preparation Products

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MPMKMQHJHDHPBE-RUZDIDTESA-N Suppliers

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1391076-61-1, MPMKMQHJHDHPBE-RUZDIDTESA-NRelated Search:


  • MPMKMQHJHDHPBE-RUZDIDTESA-N
  • GLPG 0974 (GLPG0974)
  • 4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid
  • Butanoic acid, 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-
  • GLPG0974, 10 mM in DMSO
  • 1391076-61-1