| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
LY2881835 targets GPR40/FFA1, a G-protein coupled receptor that is naturally activated by long-chain fatty acids. It is a specific GPR40 agonist with potent and selective activity. 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, LY2881835 demonstrates potent and selective agonism at GPR40. It enhances glucose-stimulated insulin secretion in normal lean mice. The compound's ability to modulate insulin secretion in response to glucose stimulation makes it a promising candidate for type 2 diabetes therapy.
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| ln Vivo |
In vivo, LY2881835 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's glucose-lowering effects and ability to enhance incretin secretion support its potential for the treatment of type 2 diabetes mellitus.
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| Enzyme Assay |
In vitro receptor binding and functional assays for GPR40 agonism involve incubating cells expressing human GPR40 with varying concentrations of LY2881835. GPR40-mediated signaling is assessed by measuring calcium mobilization, β-arrestin recruitment, or cAMP modulation. EC50 values are calculated from dose-response curves to determine the compound's potency.
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| Cell Assay |
Cellular assays are performed using cell lines expressing human GPR40. Cells are treated with LY2881835 at various concentrations, and GPR40-mediated signaling is assessed. Insulin secretion assays are performed using pancreatic β-cell lines or isolated islets to confirm the compound's ability to enhance glucose-stimulated insulin secretion.
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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. LY2881835 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 |
LY2881835 (molecular weight 493.59, formula C₃₁H₃₁NO₅) is a small-molecule compound. It is a specific GPR40 agonist with potential oral bioavailability. The compound is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have evaluated LY2881835 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-2881835 is being investigated in the clinical trial NCT01358981 (an LY2881835 study in healthy individuals and patients with diabetes).
LY2881835 is a potent and selective 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. LY2881835 is primarily used for research purposes and has not received regulatory approval for clinical use. |
| Molecular Formula |
C33H33NO3
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|---|---|
| Molecular Weight |
491.62
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| Exact Mass |
491.246
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| CAS # |
1292290-38-0
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| PubChem CID |
51049992
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
676.6±55.0 °C at 760 mmHg
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| Flash Point |
363.0±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
6.08
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
843
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(C(C1=CC=C(OCC2=CC=C(CN3CCC4(C5=C(C=CC=C5)C=C4)CC3)C=C2)C=C1)CC(O)=O)#CC
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| InChi Key |
WKVVLTUTCPYXBP-LJAQVGFWSA-N
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| InChi Code |
InChI=1S/C33H35NO3/c1-2-5-29(22-32(35)36)27-12-14-30(15-13-27)37-24-26-10-8-25(9-11-26)23-34-20-18-33(19-21-34)17-16-28-6-3-4-7-31(28)33/h3-4,6-15,29H,16-24H2,1H3,(H,35,36)/t29-/m0/s1
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| Chemical Name |
(S)-3-(4-((4-((2,3-dihydrospiro[indene-1,4'-piperidin]-1'-yl)methyl)benzyl)oxy)phenyl)hex-4-ynoic acid
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| Synonyms |
LY2881835; LY-2881835; LY 2881835.
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0341 mL | 10.1705 mL | 20.3409 mL | |
| 5 mM | 0.4068 mL | 2.0341 mL | 4.0682 mL | |
| 10 mM | 0.2034 mL | 1.0170 mL | 2.0341 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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