[CAS NO. 306974-70-9] GW-1100
PRODUCTS SPECIFICATIONS [306974-70-9]
DESCRIPTION [306974-70-9]
Overview
| MDL | MFCD09953714 |
|---|---|
| Molecular Weight | 520.58 |
| Molecular Formula | C27H25FN4O4S |
| SMILES | O=C1C(CC2=CN=C(N=C2)OCC)=CN(C(SCC3=CC=C(C=C3)F)=N1)C4=CC=C(C(OCC)=O)C=C4 |
15 Publications Citing Use of MCE
- [1]Neuropharmacology. 2020 Mar 1;164:107899.
- [2]J Agric Food Chem. 2019 Aug 21;67(33):9148-9159.
- [3]J Endocrinol. 2019 Feb 1;240(2):195-214.
- [4]Sci Rep. 2017 Jun 28;7(1):4351.
- [5]Mol Cell Endocrinol. 2022: 111836.
- [6]Am J Pathol. 2015 Jan;185(1):185-96.
- [7]Molecules. 2020 Mar 2;25(5):1102.
- [8]Eur J Pharmacol. 2021 Jul 20;174362.
- [9]Nutr Metab. 2021 Nov 21;18(1):100.
- [10]Psychopharmacology. 2021 Aug;238(8):2133-2146.
- [11]RSC Adv. 2019, 9(26):15073-15083.
- [12]J Diabetes Res. 2019 Feb 3;2019:5245063.
- [13]PLoS One. 2018 Jul 11;13(7):e0200449.
- [14]Naunyn Schmiedebergs Arch Pharmacol. 2020 Oct;393(10):1797-1808.
- [15]Braz J Pharm Sci. 2023, 58.
Summary
GW-1100 is a selective GPR40 antagonist with a pIC 50 of 6.9.
IC50 & Target
pIC50: 6.9 (GPR40) [1]
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 [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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 96.05 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9209 mL | 9.6047 mL | 19.2093 mL |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL |
| 10 mM | 0.1921 mL | 0.9605 mL | 1.9209 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 50% PBS
Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
-
3.
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: 0.06 mg/mL (0.12 mM); Suspended solution; Need ultrasonic
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.
