| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GPR109 receptor agonist-3 (Compound N2L) (10-100 μM, pretreatment for 30 minutes) significantly reduced L-glutamate-induced toxicity in HT22 cells and effectively reduced H2O2-induced toxicity in HUVECs, improving cell survival [1].
|
|---|---|
| ln Vivo |
GPR109 receptor agonist-3 (compound N2L) (60 mg/kg, orally, once daily for 4 weeks) reduced total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and increased high-density lipoprotein cholesterol (HDL-C) in high-fat diet supplementation[1]. GPR109 receptor agonist-3 (0.03%–0.1% in diet, Manhattan, 9 weeks) reduced aortic plaque area, decreased serum TC, TG, and LDL-C, increased HDL-C, reduced vascular superoxide production and cardiac MDA levels, and inhibited weight gain in ApoE knockout mice[1].
|
| Animal Protocol |
Animal/Disease Models: High-fat diet-fed rats: Female Sprague-Dawley rats were fed a high-fat diet (5% lard oil, 10% sugar and 1% cholesterol) for 8 weeks to establish hyperlipidemia model[1]
Doses: 60 mg/kg Route of Administration: p.o. daily for 4 weeks Experimental Results: Decreased total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) levels. Increased high-density lipoprotein cholesterol (HDL-C) level. Animal/Disease Models: ApoE null mice: Homozygous male apolipoprotein E (ApoE) null mice (10 weeks old) on C57BL/6 background were fed a Western-type diet containing 0.15% (w/w) cholesterol and 21% (w/w) fat for 1 week to obtain similar total cholesterol levels, then used to establish atherosclerosis model[1] Doses: 0.03% and 0.1% in diet Route of Administration: p.o. for 9 weeks Experimental Results: Reduced aortic plaque area. Decreased serum total cholesterol (TC) triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C). Increased high-density lipoprotein cholesterol (HDL-C) by 128% at 0.1% dose. Attenuated vascular superoxide production in innominate arteries. Decreased hepatic malondialdehyde (MDA) level to 36% at 0.1% dose. Inhibited body weight gain compared to control. Exhibited higher food intake but lower body weight. Showed no significant liver or kidney toxicity, with hepatic protection against diet-induced damage. |
| References |
| Molecular Formula |
C16H23N3O2S2
|
|---|---|
| Molecular Weight |
353.50
|
| CAS # |
944559-31-3
|
| Appearance |
Typically exists as solids at room temperature
|
| 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
|
|---|---|
| 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 | 2.8289 mL | 14.1443 mL | 28.2885 mL | |
| 5 mM | 0.5658 mL | 2.8289 mL | 5.6577 mL | |
| 10 mM | 0.2829 mL | 1.4144 mL | 2.8289 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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