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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
LY-2922470 targets GPR40/FFA1, a G-protein coupled receptor naturally activated by long-chain fatty acids. It is a selective and orally active agonist with EC50 values of 7 nM for human GPR40, 1 nM for mouse GPR40, and 3 nM for rat GPR40. By activating GPR40, the compound enhances glucose-stimulated insulin secretion from pancreatic β-cells and increases GLP-1 secretion.
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| ln Vitro |
In vitro, LY-2922470 activates GPR40-mediated β-arrestin recruitment with EC50 values of 7 nM (human GPR40), 1 nM (mouse GPR40), and 3 nM (rat GPR40). The compound demonstrates potent and selective agonism at GPR40, enhancing insulin and GLP-1 secretion in response to glucose stimulation.
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| ln Vivo |
In vivo, LY-2922470 demonstrated potent, efficacious, and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion during preclinical testing. The compound improves glucose tolerance and metabolic homeostasis while exhibiting good pharmacokinetic properties. By activating GPR40, it enhances insulin release without causing hypoglycemia.
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| Enzyme Assay |
In vitro receptor binding and functional assays for GPR40 agonism involve incubating cells expressing human, mouse, or rat GPR40 with varying concentrations of LY-2922470. β-Arrestin recruitment is measured using an enzyme complementation or BRET-based assay. EC50 values are calculated from dose-response curves to determine the compound's potency across species.
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| Cell Assay |
Cellular assays are performed using cell lines expressing human, mouse, or rat GPR40. Cells are treated with LY-2922470 at various concentrations, and GPR40-mediated signaling is assessed by measuring β-arrestin recruitment, calcium mobilization, or cAMP modulation. Insulin secretion assays are performed using pancreatic β-cell lines or isolated islets.
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| Animal Protocol |
In vivo studies are conducted in rodent models of type 2 diabetes, such as high-fat diet-fed mice or db/db mice. LY-2922470 is administered orally at various doses. Glucose tolerance tests are performed to assess the compound's ability to lower glucose levels. Serum insulin and GLP-1 levels are measured to confirm target engagement.
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| ADME/Pharmacokinetics |
LY-2922470 (molecular weight 445.55, formula C₂₇H₂₇NO₄S) is a small-molecule compound. It is orally active and soluble in DMSO. The compound is typically stored at -20°C. Its physicochemical properties support oral bioavailability and favorable drug-like characteristics.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated LY-2922470 in animal models. As a GPR40 agonist, its toxicity profile is related to effects on insulin secretion and metabolic regulation. The compound has demonstrated a favorable safety profile in preclinical studies, supporting its potential for type 2 diabetes treatment.
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| References | |
| Additional Infomation |
LY-2922470 is a potent, selective, and orally active GPR40/FFA1 agonist developed for the treatment of type 2 diabetes mellitus. Its mechanism involves activating GPR40, enhancing glucose-stimulated insulin secretion and GLP-1 release. The compound has demonstrated durable glucose-lowering effects in preclinical models without causing hypoglycemia. LY-2922470 has not received regulatory approval for clinical use.
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| Molecular Formula |
C28H29NO4S
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|---|---|
| Molecular Weight |
475.599166631699
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| Exact Mass |
475.181
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| CAS # |
1423018-12-5
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| PubChem CID |
71257551
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
689.1±55.0 °C at 760 mmHg
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| Flash Point |
370.5±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.626
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| LogP |
5.89
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
724
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC#C[C@@H](CC(=O)O)C1=CC=C(C=C1)OCC2=CC=C(S2)CN3CCCC4=C3C(=CC=C4)OC
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| InChi Key |
VJVDLRVFJTVWEO-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C28H29NO4S/c1-3-6-22(17-27(30)31)20-10-12-23(13-11-20)33-19-25-15-14-24(34-25)18-29-16-5-8-21-7-4-9-26(32-2)28(21)29/h4,7,9-15,22H,5,8,16-19H2,1-2H3,(H,30,31)/t22-/m0/s1
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| Chemical Name |
(S)-3-(4-((5-((8-methoxy-3,4-dihydroquinolin-1(2H)-yl)methyl)thiophen-2-yl)methoxy)phenyl)hex-4-ynoic acid
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| Synonyms |
LY2922470; LY-2922470; LY 2922470.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~262.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1026 mL | 10.5130 mL | 21.0261 mL | |
| 5 mM | 0.4205 mL | 2.1026 mL | 4.2052 mL | |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1026 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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