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
- 1. Meng-Yan Deng, Khalil Ali Ahmad, et al. "Thalidomide alleviates neuropathic pain through microglial IL-10/β-endorphin signaling pathway." Biochem Pharmacol. 2021 Oct;192:114727. PMID: 34390739
- 2. Gao, Bo, et al. "Dose-response estrogen promotes osteogenic differentiation via GPR40 (FFAR1) in murine BMMSCs." Biochimie (2015). PMID: 25576830
- 3. Gao, Bo, et al. "Ginsenoside-Rb2 inhibits dexamethasone-induced apoptosis through promotion of GPR120 induction in bone marrow-derived mesenchymal stem cells." Stem cells and development ja (2014).
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 520.59 |
| Cas No. | 306974-70-9 |
| Formula | C27H25FN4O4S |
| Synonyms | GW1100;GW1100 |
| Solubility | Soluble in DMSO |
| Chemical Name | ethyl 4-[5-[(2-ethoxypyrimidin-5-yl)methyl]-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]benzoate |
| SDF | Download SDF |
| Canonical 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
