GPR40 AgoPAM AP5

  Cat. No.:  DC11143  
Chemical Structure
1623194-37-5
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Field of application
GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM).
Cas No.: 1623194-37-5
Chemical Name: (2S,3R)-3-cyclopropyl-3-((S)-2-(2-fluoro-4-(2-methoxypyridin-4-yl)phenyl)chroman-7-yl)-2-methylpropanoic acid
SMILES: C(O)(=O)[C@H](C)[C@H](C1CC1)C1=CC2O[C@@H](C3=CC=C(C4C=CN=C(OC)C=4)C=C3F)CCC=2C=C1
Formula: C28H28FNO4
M.Wt: 461.533
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM); t demonstrates excellent in vivo efficacy with a projected human dose of 7-15 mg, shows sustained glucose lowering effect in vivo.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC9458 GW-1100 GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.
DC11143 GPR40 AgoPAM AP5 GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM).
DC11623 GPR120 agonist 4x A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.
DC11680 LY3104607 A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.
DC11682 LY2922083 A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.
DC11683 LY2881835 A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.
DC11697 AM-1638 A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.
DC11994 ZQ-16 A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.
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