BGT-002
Based on 1 Customer Validation
BGT-002 (326E) is an orally active dual ACLY inhibitor and PPARα agonist. BGT-002 reduces lipogenesis by inhibiting synthesis and promoting efflux. BGT-002 demonstrates efficacy in ameliorating metabolic dysfunction-associated steatohepatitis (MASH) and improving hyperlipidemia in vivo. BGT-002 can be used for hypercholesterolemia and MASH research.
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- Pureté: 99.35%
- CAS No.: 2127387-94-2
- Formule: C19H34O4
- Masse moléculaire:326.47
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PPARα |
BGT-002 (3-50 μmol/L, 4h) inhibits ACLY activity and suppresses lipid synthesis in primary hepatocytes isolated from mice by acting as a prodrug for its active ACLY-inhibiting CoA-thioester metabolite[2].
BGT-002 (12.5-50 μmol/L, 24 h) increases cholesterol efflux in the primary mouse hepatocytes by upregulating the ABCG5/8 transporters[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | T1/2 | AUC0-t | Tmax | Cmax |
|---|---|---|---|---|---|---|---|---|
| Dog[2] | 5 mg/kg | i.v. | 0.13 mL/min/kg | 0.29 L/kg | 26.20 h | 534.00 μg·h/mL | / | / |
| Dog[2] | 5 mg/kg | p.o. | / | / | 27.40 h | 419.00 μg·h/mL | 0.25 h | 39.60 μg/mL |
| Mice[2] | 10 mg/kg | i.v. | 1.31 mL/min/kg | 0.33 L/kg | 4.55 h | 138.00 μg·h/mL | / | / |
| Mice[2] | 10 mg/kg | p.o. | / | / | 3.79 h | 128.40 μg·h/mL | 0.13 h | 25.65 μg/mL |
BGT-002 (20 mg/kg, p.o., daily for 18 weeks) ameliorates MASH and reverses fibrosis in cynomolgus monkeys[1].
BGT-002 (10, 30, and 100 mg/kg, p.o., single dose) significantly inhibits hepatic de novo lipogenesis in fasted-refed mice[2].
BGT-002 (30 mg/kg, p.o., single dose or daily for 7 days) increases cholesterol efflux and reduces hepatic cholesterol content in high cholesterol diet-induced mice[2].
BGT-002 (7.5, 15, 20, and 30 mg/kg, p.o., daily for 2 weeks) improves hyperlipidemia in diet-induced hyperlipidemic hamsters, and spontaneously hyperlipidemic rhesus monkeys[2].
BGT-002 (15, 30, and 60 mg/kg, p.o., daily for 24 weeks) improves atherosclerosis in Western diet (WD)-induced ApoE-/- mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ob/ob mice fed with a high-fat, highfructose, high-cholesterol diet[1]
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Dosage:15, 30, and 60 mg/kg
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Administration:p.o., daily for 9 weeks
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Result: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.
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Animal Model:Ob/ob mice fed with a choline-deficient L-amino aciddefined high-fat diet (CDAA-HFD)[1]
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Dosage:15, 30, and 60 mg/kg
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Administration:p.o., daily for 9 weeks
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Result: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.
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Animal Model:MASH cynomolgus monkeys (≥8 years old)[1]
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Dosage:20 mg/kg
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Administration:p.o., daily for 18 weeks
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Result: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.
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Animal Model:C57BL/6J mice fasted for 48 h followed by refeeding for another 48h[1]
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Dosage:10, 30, and 100 mg/kg
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Administration:p.o., single dose
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Result:Reduced lipogenesis specifically in the liver but not obviously in the muscle, heart, ileum, abdominal adipose or kidney tissues.
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Animal Model:Male golden hamsters fed with a high-fat and high-cholesterol (HFHC) die[2]
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Dosage:7.5, 15 and 30 mg/kg
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Administration:p.o., daily for 2 weeks
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Result:Exhibited a dose-dependent improvement in the hypolipidemic effect.
Reduced serum TG and HDL-C levels.
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Animal Model:Male rhesus monkeys (6-20 years old) with mild or moderate hyperlipidemia for more than 2 years[2]
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Dosage:20 mg/kg
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Administration:p.o., daily for 2 weeks
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Result:Reduced plasma concentrations of TG, LDL-C and TC.
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Animal Model:ApoE-/- induced with Western diet (WD)[2]
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Dosage:15, 30, and 60 mg/kg
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Administration:p.o., daily for 24 weeks
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Result: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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2127387-94-2
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Appearance Solid
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Masse moléculaire 326.47
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Formule C19H34O4
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Color White to off-white
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SMILES
CC(CCCC/C=C/CCCCCC(C)(C(O)=O)C)(C(O)=O)C
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Synonyms
326E
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : ≥ 100 mg/mL (306.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Xie Z, et al. The enedioic acid analog 326E alleviates metabolic dysfunction-associated steatohepatitis via dual targeting at ACLY and PPARα. Cell Metab. 2025 Nov 4;37(11):2149-2166.e9. [Content Brief]
[2]. Xie Z, et al. Development of the novel ACLY inhibitor 326E as a promising treatment for hypercholesterolemia. Acta Pharm Sin B. 2023 Feb;13(2):739-753. [Content Brief]
[3]. Zhu X, et al. Simultaneous determination of BGT-002 and its acyl glucuronide metabolite ZM326E-M2 in human plasma by liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic study. J Pharm Biomed Anal. 2024 Jun 15;243:116056. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0631 mL | 15.3153 mL | 30.6307 mL | 76.5767 mL |
| 5 mM | 0.6126 mL | 3.0631 mL | 6.1261 mL | 15.3153 mL | |
| 10 mM | 0.3063 mL | 1.5315 mL | 3.0631 mL | 7.6577 mL | |
| 15 mM | 0.2042 mL | 1.0210 mL | 2.0420 mL | 5.1051 mL | |
| 20 mM | 0.1532 mL | 0.7658 mL | 1.5315 mL | 3.8288 mL | |
| 25 mM | 0.1225 mL | 0.6126 mL | 1.2252 mL | 3.0631 mL | |
| 30 mM | 0.1021 mL | 0.5105 mL | 1.0210 mL | 2.5526 mL | |
| 40 mM | 0.0766 mL | 0.3829 mL | 0.7658 mL | 1.9144 mL | |
| 50 mM | 0.0613 mL | 0.3063 mL | 0.6126 mL | 1.5315 mL | |
| 60 mM | 0.0511 mL | 0.2553 mL | 0.5105 mL | 1.2763 mL | |
| 80 mM | 0.0383 mL | 0.1914 mL | 0.3829 mL | 0.9572 mL | |
| 100 mM | 0.0306 mL | 0.1532 mL | 0.3063 mL | 0.7658 mL |
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