| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| ln Vitro |
BGT-002 (3-50 μmol/L, 4 h) inhibits ACLY activity and lipid synthesis in mouse primary hepatocytes by acting as a prodrug for its active ACLY inhibitory CoA-thioester metabolite [2]. BGT-002 (12.5-50 μmol/L, 24 h) increases cholesterol efflux in mouse primary hepatocytes by upregulating ABCG5/8 transporter [2].
|
|---|---|
| ln Vivo |
BGT-002 (15, 30, and 60 mg/kg, orally, once daily for 9 weeks) improves MASH in frozen animal models by dual opsonizing ACLY and PPARα [1]. BGT-002 (20 mg/kg, orally, once daily for 18 weeks) improves MASH and restores fibrosis in cynomolgus monkeys [1]. BGT-002 (10, 30, and 100 mg/kg, elbow, single dose) significantly inhibits de novo fat generation in the septum of diet-refeed eyebrows [2]. BGT-002 (30 mg/kg, elbow, single or once daily for 7 days) increases lumbar outflow induced by high-waisted diets and reduces lumbar hip [2]. BGT-002 (7.5, 15, 20 and 30 mg/kg, neck, once daily for 2 weeks) BGT-002 (15, 30 and 60 mg/kg, oral, once daily for 24 weeks) improved atherosclerotic thrombosis in a Western diet (WD)-induced ApoE-/- model [2].
|
| Animal Protocol |
Animal/Disease Models: Ob/ob mice fed with a high-fat, highfructose, high-cholesterol diet[1]
Doses: 15, 30, and 60 mg/kg Route of Administration: p.o., daily for 9 weeks Experimental Results: Did not significantly alter body weight or food intake. Significantly lowered MASH diet-induced elevations in ALT and AST levels and reduced plasma lipids. Notably reduced liver weight and NAS score. Significantly reduced CD68 and F4/80 levels in liver, and downregulated the expression of genes related to liver inflammation and fibrosis. Animal/Disease Models: Ob/ob mice fed with a choline-deficient L-amino aciddefined high-fat diet (CDAA-HFD)[1] Doses: 15, 30, and 60 mg/kg Route of Administration: p.o., daily for 9 weeks Experimental Results: Significantly lowered plasma TG, ALT, and AST, without changing body weight or food intake. Alleviated CDAA-HFD induced hepatic steatosis and attenuated liver fibrosis. Significantly downregulated inflammatory and fibrotic gene expression. Alleviated CDAA-HFD-induced hepatic steatosis beyond ACLY. PPARα is required to ameliorate CDAA-HFD-induced MASH. Animal/Disease Models: MASH cynomolgus monkeys (≥8 years old)[1] Doses: 20 mg/kg Route of Administration: p.o., daily for 18 weeks Experimental Results: Steadily lowered serum ALT, AST, and γ-GTT compared with the vehicle. Returned plasma total cholesterol (TC) and LDL-C to baseline over time. Reduced high-sensitivity C-reactive protein (hs-CRP), increased serum BHB and FAO levels. Resulted ACLY inhibition and PPARα activation with a safe profile. Animal/Disease Models: C57BL/6J mice fasted for 48 h followed by refeeding for another 48h[1] Doses: 10, 30, and 100 mg/kg Route of Administration: p.o., single dose Experimental Results: Reduced lipogenesis specifically in the liver but not obviously in the muscle, heart, ileum, abdominal adipose or kidney tissues. Animal/Disease Models: Male golden hamsters fed with a high-fat and high-cholesterol (HFHC) die[2] Doses: 7.5, 15 and 30 mg/kg Route of Administration: p.o., daily for 2 weeks Experimental Results: Exhibited a dose-dependent improvement in the hypolipidemic effect. Reduced serum TG and HDL-C levels. Animal/Disease Models: Male rhesus monkeys (6-20 years old) with mild or moderate hyperlipidemia for more than 2 years[2] Doses: 20 mg/kg Route of Administration: p.o., daily for 2 weeks Experimental Results: Reduced plasma concentrations of TG, LDL-C and TC. Animal/Disease Models: ApoE-/- induced with Western diet (WD)[2] Doses: 15, 30, and 60 mg/kg Route of Administration: p.o., daily for 24 weeks Experimental Results: Significantly decreased body weight gain. Significantly decreased cholesterol and LDL-C levels. Reduced expression of the inflammatory-related genes Cd68, F4/80 and IL-1β in a dose dependent manner. |
| References |
| Molecular Formula |
C19H34O4
|
|---|---|
| Molecular Weight |
326.47
|
| CAS # |
2127387-94-2
|
| Appearance |
Typically exists as solids at room temperature
|
| Synonyms |
326E
|
| 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 | 3.0631 mL | 15.3153 mL | 30.6307 mL | |
| 5 mM | 0.6126 mL | 3.0631 mL | 6.1261 mL | |
| 10 mM | 0.3063 mL | 1.5315 mL | 3.0631 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
