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| 5mg |
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| Targets |
The primary target of JTE-907 is the cannabinoid 2 (CB2) receptor. It acts as a highly selective inverse agonist, binding to the CB2 receptor and reducing its constitutive activity. The compound shows high affinity for rat (Ki = 0.38 nM), mouse (Ki = 1.55 nM), and human (Ki = 35.9 nM) CB2 receptors.
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| ln Vitro |
In vitro, JTE-907 has been shown to be a highly selective CB2 receptor inverse agonist. It binds to the CB2 receptor with high affinity and exhibits selectivity over CB1 receptors. The compound's anti-inflammatory effects have been confirmed in various in vitro models.
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| ln Vivo |
In vivo, JTE-907 exerts anti-inflammatory effects. At 10 μM, it significantly promotes insulin secretion from human islets and from Gpr55+/+ and Gpr55-/- mouse islets, accompanied by significant elevations in IP1 and [Ca2+]i. The compound's anti-inflammatory effects are thought to be mediated by an interaction between the CB2 receptor and IgE.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for JTE-907 involve studying its binding affinity for the CB2 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the CB2 receptor. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the Ki.
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| Cell Assay |
In vitro cell-based assays for JTE-907 are performed using various cell types, such as pancreatic islets and immune cells. Cells are treated with the compound, and insulin secretion, calcium signaling, and inflammatory responses are measured. The compound's effects on CB2 receptor signaling are assessed.
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| Animal Protocol |
In vivo animal experiments for JTE-907 are conducted using mouse models. The compound is administered orally, and its anti-inflammatory effects and effects on insulin secretion are assessed. The compound's effects on GPR55-independent insulin secretion are evaluated in Gpr55+/+ and Gpr55-/- mice.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of JTE-907 indicate that it is orally active. The compound has a molecular weight of 438.48 and a molecular formula of C24H26N2O6. The CAS number is 282089-49-0. It is soluble in DMSO at 100 mg/mL. Storage at 4°C is recommended.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for JTE-907 are limited. As a CB2 receptor inverse agonist, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. However, its long-term safety profile requires further evaluation.
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| References | |
| Additional Infomation |
N-(1,3-benzodioxacyclopenten-5-ylmethyl)-7-methoxy-2-oxo-8-pentoxy-1H-quinoline-3-carboxamide is a quinoline compound and also an aromatic amide.
Other information: JTE-907 is a highly selective CB2 receptor inverse agonist. It is also known as JTE 907. The compound has anti-inflammatory effects and promotes insulin secretion. Its CAS number is 282089-49-0. |
| Molecular Formula |
C24H26N2O6
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|---|---|
| Molecular Weight |
438.48
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| Exact Mass |
438.179
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| CAS # |
282089-49-0
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| PubChem CID |
9867770
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.267g/cm3
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| Boiling Point |
704.2ºC at 760mmHg
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| Flash Point |
379.7ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.59
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| LogP |
4.155
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
698
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCOC1=C(C=CC2=C1NC(=O)C(=C2)C(=O)NCC3=CC4=C(C=C3)OCO4)OC
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| InChi Key |
GRAJFFFXJYFVOC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26N2O6/c1-3-4-5-10-30-22-19(29-2)9-7-16-12-17(24(28)26-21(16)22)23(27)25-13-15-6-8-18-20(11-15)32-14-31-18/h6-9,11-12H,3-5,10,13-14H2,1-2H3,(H,25,27)(H,26,28)
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| Chemical Name |
N-(1,3-benzodioxol-5-ylmethyl)-7-methoxy-2-oxo-8-pentoxy-1H-quinoline-3-carboxamide
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| Synonyms |
JTE907; JTE 907; JTE-907
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 (~285.08 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 | 2.2806 mL | 11.4030 mL | 22.8061 mL | |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5612 mL | |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 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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