2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. ATP Citrate Lyase PPAR
  4. BGT-002

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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BGT-002

BGT-002 Chemical Structure

CAS No. : 2127387-94-2

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Based on 1 publication(s) in Google Scholar

BGT-002 Related Antibodies

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Description

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[1][2][3].

IC50 & Target[1]

PPARα

 

In Vitro

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.

BGT-002 Related Antibodies
Parmacokinetics
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
In Vivo

BGT-002 (15, 30, and 60 mg/kg, p.o., daily for 9 weeks) ameliorates MASH in rodent models via dual targeting at ACLY and PPARα[1].
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.

Animal Model: Ob/ob mice fed with a high-fat, highfructose, high-cholesterol diet[1]
Dosage: 15, 30, and 60 mg/kg
Administration: p.o., daily for 9 weeks
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.
Animal Model: Ob/ob mice fed with a choline-deficient L-amino aciddefined high-fat diet (CDAA-HFD)[1]
Dosage: 15, 30, and 60 mg/kg
Administration: p.o., daily for 9 weeks
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.
Animal Model: MASH cynomolgus monkeys (≥8 years old)[1]
Dosage: 20 mg/kg
Administration: p.o., daily for 18 weeks
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.
Animal Model: C57BL/6J mice fasted for 48 h followed by refeeding for another 48h[1]
Dosage: 10, 30, and 100 mg/kg
Administration: p.o., single dose
Result: Reduced lipogenesis specifically in the liver but not obviously in the muscle, heart, ileum, abdominal adipose or kidney tissues.
Animal Model: Male golden hamsters fed with a high-fat and high-cholesterol (HFHC) die[2]
Dosage: 7.5, 15 and 30 mg/kg
Administration: p.o., daily for 2 weeks
Result: Exhibited a dose-dependent improvement in the hypolipidemic effect.
Reduced serum TG and HDL-C levels.
Animal Model: Male rhesus monkeys (6-20 years old) with mild or moderate hyperlipidemia for more than 2 years[2]
Dosage: 20 mg/kg
Administration: p.o., daily for 2 weeks
Result: Reduced plasma concentrations of TG, LDL-C and TC.
Animal Model: ApoE-/- induced with Western diet (WD)[2]
Dosage: 15, 30, and 60 mg/kg
Administration: p.o., daily for 24 weeks
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.
Clinical Trial
Molecular Weight

326.47

Formula

C19H34O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(CCCC/C=C/CCCCCC(C)(C(O)=O)C)(C(O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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BGT-002 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BGT-0022127387-94-2326EBGT002BGT 002ATP Citrate LyasePPARACLYPeroxisome proliferator-activated receptorsPPARαlipogenesismetabolic dysfunction-associated steatohepatitishypercholesterolemiahamstershyperlipidemic rhesus monkeyshigh cholesterol diet-induced miceInhibitorinhibitorinhibit

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