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
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
N-Bromosuccinimide Price
- Product number
- SML2443
- Product name
- GLPG0974
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $159
- Updated
- 2025/07/31
- Product number
- SML2443
- Product name
- GLPG0974
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $633
- Updated
- 2025/07/31
- Product number
- 28108
- Product name
- GLPG0974
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 28108
- Product name
- GLPG0974
- Packaging
- 5mg
- Price
- $135
- Updated
- 2024/03/01
- Product number
- G411803
- Product name
- GLPG0974
- Packaging
- 2.5mg
- Price
- $260
- Updated
- 2021/12/16
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
MPMKMQHJHDHPBE-RUZDIDTESA-N Suppliers
- Tel
- 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3506
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4757
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 71826
- Advantage
- 60
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8000
- Advantage
- 62
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9119
- Advantage
- 58
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- 86-571-88216897,88216896 13588875226
- Fax
- 86-571-88216895
- sales@hzclap.com
- Country
- CHINA
- ProdList
- 6312
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58