AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with IC50 of 117 nM. AR420626 inhibits nicotine and serotonin induced changes in motility of isolated muscle strips from rat colon. AR420626 also suppresses serotonin-induced fecal output in rats.
|Solubility (25°C)||DMSO 15 mg/mL (ultrasonic and warming)|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Related GPR/FFAR Products|
GSK256073 is a potent, selective, orally active GPR109A agonist and a potent and persistent HCA2 agonist with a pEC50 of 7.5 (Human HCA2). In addition, GSK256073 significantly improves glucose homeostasis by inhibiting lipid degradation and has potential for the study of type 2 diabetes mellitus (T2DM) and dyslipidemia.
GSK4381406 is a first-in-class, orally active GPR35 agonist for studies related to inflammatory bowel disease (IBD).
EVO756 is a Mas-related G protein-coupled receptor X2 (MRGPRX2) antagonist that can be used in studies related to urticaria.
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|hMCH-1R antagonist 1
hMCH-1R antagonist 1 is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM.
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