| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GPR61 inverse agonist 3 (compound 23) effectively inhibited the constitutive activity of human GPR61 induced by TREx in CHO cells with an IC50 value of 4.0 nM and a binding constant Ki of 0.34 nM [1]. GPR61 inverse agonist 3 also effectively inhibited the constitutive activity of mouse GPR61 in CHO cells with an IC50 value of 8.8 nM and a binding constant Ki of 1.1 nM [1]. GPR61 inverse agonist 3 exhibited moderate MDR1 efflux, low BCRP efflux, good passive permeability, and high intrinsic clearance in human hepatocytes, with corresponding values of 7.4, 1.2, 32 × 10⁻⁶ cm/s, and 152 μL/min/million cells, respectively [1]. GPR61 reverse agonist 3 (10 μM) is highly selective for GPR61, with only moderate off-target activity for GABAA chloride channels (IC50 = 4.6 μM) and PDE3A1 (IC50 = 8.9 μM), and no significant activity for 104 other targets or tested ion channels [1].
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|---|---|
| ln Vivo |
GPR61 inverse agonist 3 (compound 23) (300 mg/kg; oral; single dose) and ABT pretreatment did not produce a statistically significant increase in 24-hour cumulative food intake in 10-11 week old mice [1].
|
| Animal Protocol |
Animal/Disease Models:Mice (10-11 weeks old)[1]
Doses: 300 mg/kg Route of Administration: Oral; single administration (administered 2 hours after ABT pretreatment) Experimental Results: Compared with the vector control group, there was no statistically significant increase in the cumulative food intake over 24 hours. |
| References |
| Molecular Formula |
C21H23CLF2N6O4S
|
|---|---|
| Molecular Weight |
528.96
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COCCN(S(=O)(C1=CC=C(N=C1OC)NCC2=C(C=NC=C2F)F)=O)C3=NC(C)=C(C(C)=N3)Cl
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 1.8905 mL | 9.4525 mL | 18.9050 mL | |
| 5 mM | 0.3781 mL | 1.8905 mL | 3.7810 mL | |
| 10 mM | 0.1891 mL | 0.9453 mL | 1.8905 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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