| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SSTR5/TGR5 regulator-1 (compound 19) (cAMP assay 30 min; calcium assay pre-incubation 10 min) effectively activated human TGR5 (EC50=5.91 nM) and antagonized human SSTR5 (IC50=4.37 nM) in vitro [1]. SSTR5/TGR5 regulator-1 (cAMP assay 30 min; calcium assay pre-incubation 10 min) showed similar cross-species efficacy, activating mouse TGR5 (EC50=3.40-5.30 nM) and antagonizing mouse SSTR5 (IC50=2.97-19.6 nM) in vitro [1]. SSTR5/TGR5 regulator-1 (1 μM; maximum duration of action 60 min) showed rapid metabolic turnover in vitro, with a half-life of 2.2 min in human liver microsomes and 2.8 min in mouse liver microsomes [1]. SSTR5/TGR5 regulator-1 (30-100 μM; duration of action 24 hours) was non-toxic to primary hepatocytes at a concentration of 30 μM, but induced significant cytotoxicity after incubation at a concentration of 100 μM for 24 hours [1].
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|---|---|
| ln Vivo |
SSTR5/TGR5 modulator-1 (compound 19) (10–100 mg/kg; orally; single dose) dose-dependently improved oral glucose tolerance in male C57BL/6 mice, with the 100 mg/kg dose group showing better efficacy than the 50 mg/kg positive control group [1]. Compared with TGR5 agonist monotherapy, SSTR5/TGR5 modulator-1 (100 mg/kg; orally; single dose) attenuated TGR5-mediated gallbladder filling in male C57BL/6 mice [1]. SSTR5/TGR5 modulator-1 (100 mg/kg; orally; single dose) enhanced the GLP-1-insulin axis in male C57BL/6 mice, supporting its hypoglycemic mechanism [1].
|
| Cell Assay |
Cytotoxicity assay [1]
Cell Types: Primary hepatocytes Tested Concentrations: 30 μM; 100 μM Incubation Duration: 24 hours Experimental Results: Significant cytotoxicity was induced at 100 μM. No significant toxicity was observed at 30 μM. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (8-week-old male, approximately 25 g) [1]
Doses: 10 mg/kg; 30 mg/kg; 100 mg/kg Route of Administration: Oral; Single dose Experimental Results: Showed dose-dependent glycemic inhibition. The 100 mg/kg dose group was superior to the 50 mg/kg positive control compound 2. Compared with the solvent control group, the area under the plasma glucose curve (AUC0-90 min) was significantly reduced in all tested dose groups. Animal/Disease Models:C57BL/6 (8-week-old males) [1] Doses: 100 mg/kg Route of Administration: Oral; single dose Experimental Results: Compared with the carrier control subgroup that was not stimulated by egg yolk and the compound 2 (50 mg/kg) treatment group, the gallbladder volume was reduced, indicating that it had a weak effect on gallbladder filling. |
| References |
| Molecular Formula |
C39H45N5O7S
|
|---|---|
| Molecular Weight |
727.87
|
| CAS # |
3069267-46-2
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C([C@H]1N(CSC1)CC2=C(C=C(C(OC)=C2)CN3CCC4(CC3)OC(N(C4)C5=CC=C(C=C5)C(O)=O)=O)OC)N6CCN(C7=C6C=CC=C7)C8CC8
|
| 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 | 1.3739 mL | 6.8694 mL | 13.7387 mL | |
| 5 mM | 0.2748 mL | 1.3739 mL | 2.7477 mL | |
| 10 mM | 0.1374 mL | 0.6869 mL | 1.3739 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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