SML2443
GLPG0974
≥98% (HPLC)
동의어(들):
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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모든 사진(1)
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5 MG
₩231,928
25 MG
₩931,263
About This Item
실험식(Hill 표기법):
C25H25ClN2O4S
CAS Number:
Molecular Weight:
485.00
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
광학 활성
[α]/D +175 to +200°, c = 1 in chloroform-d
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
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
생화학적/생리학적 작용
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 Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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시험 성적서(COA)
Lot/Batch Number
이미 열람한 고객
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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