AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM.
|Source||Physiol Rep (2015). Figure 3. AMG-837|
|Cell Lines||rat small intestine|
|Results||Intergroup comparisons between LA, TAK-875, AMG 837, and DMSO stimulations showed that only the GLP-1 response induced by vascular AMG 837 was significantly different from the vehicle control|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Related GPR Products|
AF64394 is a selective GPR3 inverse agonist with a pIC50 of 7.3.
GTPL5846 (6-OAU) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120).
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
ONC212, a fluorinated-ONC201 analogue, is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.