| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Free fatty acid receptor 1 (FFA1/GPR40).
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|---|---|
| ln Vitro |
Caspases-3/7 are often less likely to be activated by GPR40 agonists 4 [1].
INVIVO6574 activates GPR40 with a pEC50 of 7.54. By agonizing GPR40, it enhances glucose-stimulated insulin secretion from pancreatic β-cells. Detailed functional activity data are available in primary publications. |
| ln Vivo |
Compound 20, also known as GPR40 agonist 4, was delivered orally once, and it was found to boost insulin production and considerably reduce plasma glucose excursions during an oral glucose tolerance test (OGTT) in a dose-dependent manner ranging from 1 to 10 mg/kg. minutes before to the oral glucose test. The blood glucose and blood insulin area under the curves (AUC0-120min) indicated that 3 mg/kg was the lowest effective dose of GPR40 agonist 4. Additionally, there was a considerable improvement in the hyperglycemic condition of the GPR40 agonist 4 (20 mg/kg) treatment group [1].
INVIVO6574 promotes insulin production in a dose-dependent manner. In oral glucose tolerance tests (OGTT), it significantly reduces plasma glucose excursion at doses of 1 to 10 mg/kg when administered before oral glucose challenge. The compound is used to study GPR40 biology and as a potential therapeutic for type 2 diabetes. |
| Enzyme Assay |
GPR40 receptor activation is measured using calcium flux assays or reporter gene assays. Cells expressing human GPR40 are loaded with calcium-sensitive dyes and treated with varying concentrations of INVIVO6574. Changes in intracellular calcium are measured fluorometrically to determine pEC50 values.
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| Cell Assay |
Pancreatic β-cell lines or primary islets are treated with INVIVO6574 at various concentrations in the presence of glucose. Insulin secretion is measured by ELISA or immunoassay. Glucose-stimulated insulin secretion (GSIS) enhancement is assessed. Cell viability is evaluated to ensure compound non-toxicity.
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| Animal Protocol |
INVIVO6574 is evaluated in rodent models of diabetes and glucose intolerance. Animals undergo oral glucose tolerance tests (OGTT) with or without INVIVO6574 administration. Blood glucose and plasma insulin levels are measured over time. The compound is administered orally at doses of 1 to 10 mg/kg.
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| ADME/Pharmacokinetics |
INVIVO6574 has molecular weight 416.87 and formula C21H17ClO5S. As a small-molecule GPR40 agonist, it is suitable for oral administration. Detailed PK parameters (half-life, bioavailability, clearance) are available in primary research publications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for INVIVO6574 are limited. As a GPR40 agonist, potential on-target effects may include modulation of insulin secretion and lipid metabolism.
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| References | |
| Additional Infomation |
INVIVO6574 is a research tool for studying GPR40 biology, glucose homeostasis, and type 2 diabetes. Its mechanism involves agonizing GPR40, enhancing glucose-stimulated insulin secretion from pancreatic β-cells. No clinical trials or approved indications exist.
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| Molecular Formula |
C21H17CLO5S
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|---|---|
| Molecular Weight |
416.874684095383
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| Exact Mass |
416.048
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| CAS # |
2102196-57-4
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| PubChem CID |
131842087
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
609
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC=CC=1C1=CC=CC(=C1)COC1C=CC(=CC=1)S(CC(=O)O)(=O)=O
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| InChi Key |
YEFZZALZTNOYEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17ClO5S/c22-20-7-2-1-6-19(20)16-5-3-4-15(12-16)13-27-17-8-10-18(11-9-17)28(25,26)14-21(23)24/h1-12H,13-14H2,(H,23,24)
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| Chemical Name |
2-[4-[[3-(2-chlorophenyl)phenyl]methoxy]phenyl]sulfonylacetic acid
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| Synonyms |
FAA1 agonist1; FAA1 agonist 1; FAA1 agonist-1
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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) |
DMSO : ~160 mg/mL (~383.81 mM)
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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 | 2.3988 mL | 11.9941 mL | 23.9883 mL | |
| 5 mM | 0.4798 mL | 2.3988 mL | 4.7977 mL | |
| 10 mM | 0.2399 mL | 1.1994 mL | 2.3988 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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