| Identification | Back Directory | [Name]
GW-1100 | [CAS]
306974-70-9 | [Synonyms]
GW-1100
GW1100;GW1100
GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem
1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone
Benzoic acid, 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-, ethyl ester | [Molecular Formula]
C27H25FN4O4S | [MDL Number]
MFCD09953714 | [MOL File]
306974-70-9.mol | [Molecular Weight]
520.58 |
| Chemical Properties | Back Directory | [Melting point ]
208-210℃ | [Boiling point ]
690.2±65.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
Soluble in DMSO (up to 2 mg/ml) or in DMF (up to 5 mg/ml). | [form ]
White powder | [pka]
1.20±0.22(Predicted) | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. Dilutions into aqueous media are not stable and should be used within one working day. |
| Hazard Information | Back Directory | [Description]
GW1100 (306974-70-9) is a selective antagonist of GPR40. GW1100 inhibits GRP40-mediated Ca2+?increases stimulated by GW9508 (Cat.# 10-1108) or linoleic acid (pIC50?= 5.99 for either agonist).1?The effects of GPR40 activation on insulin secretion in cells are also blocked by the addition of GW1100. GW1100 does not influence calcium mobilization mediated by GPR120. | [Uses]
GW 1100 is a selective G protein-coupled receptor GPR40 antagonist. GW 1100 has been shown to reverse the effects GPR40 agonists which induce glucose-stimulated insulin secretion. | [Biological Activity]
GW-1100 is a selective GPR40 antagonist with pIC50 of 6.9. | [in vitro]
GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC 50 =7.17±0.08 in the absence and pEC 50 =6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC 50 response. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC (60-150 s) , p<0.05), 100 μM linoleic acid (AUC (60-150 s) , p<0.05) and 10 μM GW9508 (AUC (60-150 s) , p<0.05). | [in vivo]
The intracerebroventricular injection of DHA (50 μg) and GW9508 (1.0 μg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 μg), a GPR40 antagonist. | [storage]
Store at -20°C | [References]
1) Brisco?et al. (2006),?Pharmacological regulation of insulin secretion in MIN6 cells through fatty acid receptor GPR40: identification of agonist and antagonist molecules; Br. J. Pharmacol.,?148?619
2) Nagatake?et al. (2018),?The 17,18-Epoxytetraenoic acid-G protein-coupled receptor 40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques; J. Allergy Clin. Immunol.,?142?470 [Focus Biomolecules Citation] |
|
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
|