Product Details
| Product Name:
AM-4668 |
CAS No.:
1011531-27-3 |
| Purity:
99.92% |
Supply Ability:
10g |
| Release date:
2026/05/11 |
Product Introduction
Bioactivity
| Name | AM-4668 |
| Description | AM-4668, a GPR40 (FFA1) agonist with oral availability, was optimized to reduce central nervous system (CNS) permeability, with a mouse brain/plasma ratio of only 0.02, and significantly reduced blood glucose levels in human GPR40 knock-in mice. |
| In vitro | The in vitro activity of AM-4668 was evaluated in CHO and A9 cells stably expressing human GPR40, showing potent agonist activity with EC?? values of 2.6?nM (aequorin assay) and 8.4?nM (IP? accumulation assay). In islets isolated from human GPR40 knock-in mice, AM-4668 stimulated insulin secretion with an EC?? of 55?nM. AM-4668 also showed minimal toxicity in CYP inhibition and hERG channel assays and exhibited low CNS penetration (brain-to-plasma ratio of 0.02 at 3?h after oral dosing at 5?mg/kg in rats)[1]. |
| In vivo | The in vivo activity of AM-4668 was tested in human GPR40 knock-in mice. Mice were fasted for 6 hours and orally administered AM-4668 (10?mg/kg); one hour later, they underwent an oral glucose tolerance test (2?g/kg). AM-4668 reduced the glucose area under the curve (AUC) by 19% compared to vehicle controls. The compound also exhibited favorable pharmacokinetics in rats, dogs, and cynomolgus monkeys, with low clearance (0.04–0.15?L/h/kg), moderate to long half-life (5.3–14?h), and good oral bioavailability (65–100%) [1]. |
| Storage | Store at low temperature,Keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | GPR40 | AM-4668 | AM 4668 |
| Inhibitors Related | Monomethyl fumarate | Kynurenic acid | Pamoic acid disodium | Azathioprine | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | TUG-424 | Timapiprant |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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