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SML2443

Sigma-Aldrich

GLPG0974

≥98% (HPLC)

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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
Empirical Formula (Hill Notation):
C25H25ClN2O4S
CAS Number:
Molecular Weight:
485.00
MDL number:

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

SMILES string

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

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SML2412SML2793SML1890
GLPG0974 ≥98% (HPLC)

SML2443

GLPG0974

EU1794-4 ≥98% (HPLC)

SML2412

EU1794-4

ZJ43 ≥98% (HPLC)

SML2793

ZJ43

MK204 ≥98% (HPLC)

SML1890

MK204

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 3 mg/mL, clear (warmed)

color

white to beige

color

white to beige

color

white to beige

color

white to beige

optical activity

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

optical activity

-

optical activity

-

optical activity

-

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.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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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