| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TMN-OMe (5 nM - 33.3 μM; 2 h) activated human GPR39 expressed in CHO-K1 cells in a β-arrestin recruitment assay, with an EC50 of 1.65 μM[1].
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|---|---|
| ln Vivo |
[11C]TMN-OMe (8.5 MBq; intravenous injection; single bolus injection) can rapidly penetrate the blood-brain barrier and specifically bind to GPR39 in healthy male BALB/c mice, whose baseline brain SUV value is 0.31 g/mL, which can be reduced by up to 86.8% under blocking conditions [1]. [11C]TMN-OMe (8.5 MBq; intravenous injection; single bolus injection) can detect a decrease in GPR39 levels in the brains of APP/PS1 Alzheimer's disease model mice [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 6 months old); GPR39 knockout mice (male, 6 months old) [1]
Doses: 8.5 MBq Route of Administration: Intravenous injection; single bolus injection Experimental Results: Wild-type mice had a brain uptake of 0.31 g/mL SUV, while GPR39 knockout mice had a brain uptake of 0.09 g/mL SUV, a reduction of 69.4%. 30 minutes after injection, wild-type mice had a brain uptake of 1.01 %ID/g, while GPR39 knockout mice had a brain uptake of 0.29 %ID/g, a reduction of 71%. Ex vivo autoradiography showed that the brain uptake of wild-type mice was 6.35 PSL/mm2, while that of GPR39 knockout mice was 4.58 PSL/mm2, a decrease of 27%. Animal/Disease Models: APP/PS1 transgenic mice (male, 6 months old); wild-type mice (male, 6 months old)[1] Doses: 8.5 MBq Route of Administration: Intravenous injection; single bolus injection Experimental Results: The brain uptake of APP/PS1 transgenic mice reached 0.15 g/mL SUV, while the brain uptake of wild-type mice was 0.29 g/mL SUV, a decrease of 46.8%. |
| References |
| Molecular Formula |
C19H16CLN7O2
|
|---|---|
| Molecular Weight |
409.83
|
| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC1=NN(C(N2)=C1C(C3=C(Cl)C=C(OC)C=C3)CC2=O)C4=NC=NC5=C4N=CN5
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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 | 2.4400 mL | 12.2002 mL | 24.4004 mL | |
| 5 mM | 0.4880 mL | 2.4400 mL | 4.8801 mL | |
| 10 mM | 0.2440 mL | 1.2200 mL | 2.4400 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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