GW-1100

GPR40 antagonist CAS# 306974-70-9

GW-1100

Catalog No. BCC1610----Order now to get a substantial discount!

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Quality Control of GW-1100

Number of papers citing our products

Chemical structure

GW-1100

3D structure

Chemical Properties of GW-1100

Cas No. 306974-70-9 SDF Download SDF
PubChem ID 11692123 Appearance Powder
Formula C27H25FN4O4S M.Wt 520.59
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (96.05 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name ethyl 4-[5-[(2-ethoxypyrimidin-5-yl)methyl]-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]benzoate
SMILES CCOC1=NC=C(C=N1)CC2=CN(C(=NC2=O)SCC3=CC=C(C=C3)F)C4=CC=C(C=C4)C(=O)OCC
Standard InChIKey PTPNCCWOTBBVJR-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H25FN4O4S/c1-3-35-25(34)20-7-11-23(12-8-20)32-16-21(13-19-14-29-26(30-15-19)36-4-2)24(33)31-27(32)37-17-18-5-9-22(28)10-6-18/h5-12,14-16H,3-4,13,17H2,1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GW-1100

DescriptionGW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. GW1100 acts as a GPR40 inverse agonist.In Vitro:GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid (pIC50 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 (pEC50=7.17±0.08 in the absence and pEC50=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 pEC50 response[2]. 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)[3].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[4].

References:
[1]. Stoddart LA, et al. Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist. Mol Pharmacol. 2007 Apr;71( [2]. Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28. [3]. Manosalva C, et al. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils. PLoS One. 2015 Mar 19;10(3):e0119715. [4]. Nakamoto K, et al. Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatorychronic pain. PLoS One. 2013 Dec 12;8(12):e81563.

Protocol

Cell Assay [3]
CHO-K1/bFFAR1 or CHO-K1/pcDNA3.1 cells (2×106 cells/2 mL) are loaded with 2.5 μM Fura-2AM fluorescent indicator dye in recording buffer (10 mM HEPES, 140 mM NaCl, 2 mM CaCl2, 21 mM MgCl2, 25 mM KCl, 10 mM glucose, pH 7.4) for 30 min, washed three times with recording buffer, and returned to the incubator for 10 min. Cells are incubated with different concentrations of propionic acid (1, 10 and 30 mM), oleic acid (0-500 μM), linoleic acid (0-200 μM), GW9508 (0-100 μM), ionomycin (2 μM), thapsigargin (2 μM) or vehicle (0.1% DMSO). The fatty acid concentrations used in all experiments are in the range of concentrations of healthy and peripartum cows. In another set of experiments, cells are incubated with either 10 μM GW-1100 for 15 min, 2 μM U73122 for 3 min or vehicle (0.1% DMSO) for 15 min and then stimulated with either 300 μM oleic acid, 100 μM linoleic acid or 10 μM GW9508. Cellular fluorescence (Ca2+) is measured at 509 nm emission with 340/380 nm dual wavelength excitation using a LS55 spectrofluorimeter. Cuvette temperatures are maintained at 37°C with constant stirring[3].

Animal Administration [4]
Mice[4] Male ddY mice (age, 4 weeks) are housed in cages at 23-24°C with a 12-h light-dark cycle (lights from 8 am to 8 pm) and food and waterad libitum. DHA (50 µg/mouse), the selective GPR40-agonist GW9508 (1.0-25 µg/mouse) and the GPR40 antagonist GW1100 (1-10 µg/mouse) are dissolved in 1% DMSO and the solution is diluted with saline before von Frey testing (1% DMSO final concentration). The doses of GW9508 are chosen based upon our previous publication, whereas GW-1100 is selected on the basis of previous reports and our preliminary experiments. Under a non-anesthetized state, DHA and GW9508 are administered via the intracerebroventricular (i.c.v.) route 10 min before CFA injection, and GW1100 is administered via the i.c.v. route 10 min before GW9508 injection. Flavopiridol (5 and 15 nmol/mouse), a cyclin-dependent kinase inhibitor, is administered by i.c.v. injection into the left lateral ventricle of the mice twice a day (at 9:00 and 19:00) after CFA treatment.

References:
[1]. Stoddart LA, et al. Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist. Mol Pharmacol. 2007 Apr;71( [2]. Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28. [3]. Manosalva C, et al. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils. PLoS One. 2015 Mar 19;10(3):e0119715. [4]. Nakamoto K, et al. Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatorychronic pain. PLoS One. 2013 Dec 12;8(12):e81563.

GW-1100 Dilution Calculator

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GW-1100 Molarity Calculator

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Preparing Stock Solutions of GW-1100

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9209 mL 9.6045 mL 19.209 mL 38.4179 mL 48.0224 mL
5 mM 0.3842 mL 1.9209 mL 3.8418 mL 7.6836 mL 9.6045 mL
10 mM 0.1921 mL 0.9604 mL 1.9209 mL 3.8418 mL 4.8022 mL
50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.7684 mL 0.9604 mL
100 mM 0.0192 mL 0.096 mL 0.1921 mL 0.3842 mL 0.4802 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GW-1100

GW1100 is a selective GPR40 antagonist. It dose dependently inhibited GPR40-mediated Ca2+ elevations stimulated by GW9508 and linoleic acid with pIC50 values of 5.9970.03 and 5.9970.06, respectively 1.

GW1100 inhibited the Ca2+ elevations stimulated by GW9508 mediated by GPR40, but not those mediated via GPR120 by either GW9508 or linoleic acid, demonstrating that GW1100 was a selective antagonist of the GPR40 receptor. GW1100 reversed the effects of GW9508 on insulin secretion, but only partially attenuated linoleic acid-stimulated insulin secretion 1. Ishikawa cells were treated with a GPR40 antagonist, GW1100, in conjunction with GW9508. GW1100 had no effect on the stimulation of cell proliferation, suggesting all pro-proliferative effects of GW9508 are mediated through GPR120 2.

References:
1. Briscoe CP, Peat AJ, McKeown SC et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28.
2. http://www.aups.org.au/Proceedings/41/44P

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Description

GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.

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