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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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Size/SKUAvailabilityPrice
5 mg

Estimated to ship TODAYfromMILWAUKEE

$176.00
25 mg

Estimated to ship TODAYfromMILWAUKEE

$704.00

About This Item

Empirical Formula (Hill Notation):
C25H25ClN2O4S
CAS Number:
Molecular Weight:
485.00
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder

$176.00


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Product Name

GLPG0974, ≥98% (HPLC)

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

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

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.

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This Item
SML3428HTS063RTA
description

≥98% (HPLC)

description

≥97% (HPLC)

description

-

form

powder

form

powder

form

-

assay

≥98% (HPLC)

assay

≥97% (HPLC)

assay

-

storage temp.

2-8°C

storage temp.

-10 to -25°C

storage temp.

-

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

-

color

white to beige

color

white to beige

color

-

optical activity

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

optical activity

-

optical activity

-


Storage Class

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable



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