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CN

SML2443

GLPG0974

≥98% (HPLC), FFA2/FFAR2/GPCR43/GPR43 antagonist , powder

Synonym(s):

4-[[(R)-1-(Benzo[b]thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl]-(3-chloro-benzyl)-amino]-butyric acid, GLPG 0974, GLPG-0974

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About This Item

Empirical Formula (Hill Notation):
C25H25ClN2O4S
CAS Number:
1391076-61-1
Molecular Weight:
485.00
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28502087

Key Documents

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Product Name

GLPG0974, ≥98% (HPLC)

InChI

1S/C25H25ClN2O4S/c1-25(11-13-28(25)23(31)20-16-33-21-9-3-2-8-19(20)21)24(32)27(12-5-10-22(29)30)15-17-6-4-7-18(26)14-17/h2-4,6-9,14,16H,5,10-13,15H2,1H3,(H,29,30)/t25-/m1/s1

InChI key

MPMKMQHJHDHPBE-RUZDIDTESA-N

SMILES string

O=C(C1=CSC2=C1C=CC=C2)N3CC[C@]3(C)C(N(CC4=CC=CC(Cl)=C4)CCCC(O)=O)=O

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +175 to +200°, c = 1 in chloroform-d

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Related Categories

Biochem/physiol Actions

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.).
Orally available, high-affinity, potent and selective free fatty acid receptor 2 (FFA2; FFAR2; GPCR43; GPR43) antagonist with in vitro and in vivo efficacy.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000209598
0000209598
0000165994
0000155052
0000155051

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Amira Sayed Khan et al.
Cellular and molecular gastroenterology and hepatology, 15(3), 633-663 (2022-11-22)
The spontaneous preference for dietary lipids is principally regulated by 2 lingual fat taste receptors, CD36 and GPR120. Obese animals and most of human subjects exhibit low orosensory perception of dietary fat because of malfunctioning of these taste receptors. Our
Xianzhang Zeng et al.
Microbiome, 11(1), 204-204 (2023-09-12)
Aging is a significant risk factor for ischemic stroke and worsens its outcome. However, the mechanisms for this worsened neurological outcome with aging are not clearly defined. Old C57BL/6J male mice (18 to 20 months old) had a poorer neurological

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