2. Metabolic Enzyme/Protease GPCR/G Protein
  3. ACSL Family GLP Receptor
  4. LP-856866

LP-856866 is an orally active ACSL5 inhibitor, with IC50 values of 8 nM and 4 nM against mouse and human ACSL5, respectively, and IC50 values of 6 nM and 17 nM against mouse and human ACSL1, respectively. LP-856866 induces delayed gastric emptying, promotes GLP-1 release, reduces food intake, decreases body weight and body fat mass, preserves lean body mass, improves glucose homeostasis, enhances insulin sensitivity, reduces hepatic lipid accumulation, and lowers serum triglyceride and total cholesterol levels. LP-856866 is applicable to research on diet-induced obesity.

For research use only. We do not sell to patients.

LP-856866

LP-856866 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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ACSL4 ACSL5

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Description

LP-856866 is an orally active ACSL5 inhibitor, with IC50 values of 8 nM and 4 nM against mouse and human ACSL5, respectively, and IC50 values of 6 nM and 17 nM against mouse and human ACSL1, respectively. LP-856866 induces delayed gastric emptying, promotes GLP-1 release, reduces food intake, decreases body weight and body fat mass, preserves lean body mass, improves glucose homeostasis, enhances insulin sensitivity, reduces hepatic lipid accumulation, and lowers serum triglyceride and total cholesterol levels. LP-856866 is applicable to research on diet-induced obesity[1].

IC50 & Target

ACSL5

 

In Vivo

LP-856866 (10-60 mg/kg/day; p.o.; continuous dietary admixture; 28 days) induces dose-dependent body weight and body fat loss with preserved lean body mass, and improves glucose tolerance and insulin sensitivity in male diet-induced obesity mice[1].
LP-856866 (p.o.; dietary admixture) reduces high-fat diet consumption in wild-type mice but not Acsl5 knockout mice, confirming targeted ACSL5 inhibition[1].
LP-856866 (75 mg/kg/day; p.o.; continuous dietary admixture; 11 days) shifts dietary preference away from high-fat diet, reduces total caloric intake, and prevents weight gain in male mice given access to both low-fat and high-fat diets[1].
LP-856866 (60 mg/kg/day; p.o.; continuous dietary admixture; 17 days) reduces hepatic triglyceride levels in male Mus musculus fed a high-fat diet[1].
LP-856866 (60 mg/kg/day; p.o.; continuous dietary admixture; 3 weeks) reduces serum total cholesterol and triglyceride levels in male Mus musculus fed a high-fat diet[1].
LP-856866 (60 mg/kg; p.o.; single pretreatment dose; 30 minutes before HFD meal) increases postprandial active GLP-1 levels in male mice, with a synergistic effect when combined with sitagliptin[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; diet-induced obesity model, fed 45% high-fat diet from weaning for over 16 weeks)[1]
Dosage: 10 mg/kg/day; 30 mg/kg/day; 60 mg/kg/day
Administration: p.o.; continuous dietary admixture; 28 days
Result: Induced significant, dose-dependent body weight loss and body fat loss with reduced lean body mass loss compared to vehicle-treated mice at 28 days.
Lowered glucose excursions at 30 minutes significantly in 30 mg/kg/day and 60 mg/kg/day groups compared to vehicle-treated mice during OGTT.
Reduced insulin excursions at 30 and 60 minutes significantly in all treated groups compared to vehicle-treated mice during OGTT.
Improved Homeostatic Model Assessment Insulin Sensitivity Index (HOMA ISI) and Composite ISI significantly in all treated groups compared to vehicle-treated mice.
Animal Model: C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; chow-fed, acclimated to 10% low-fat diet for 2 weeks)[1]
Dosage: 75 mg/kg/day
Administration: p.o.; continuous dietary admixture; 11 days
Result: Increased daily intake of 10% low-fat diet significantly and decreased daily intake of 60% high-fat diet significantly compared to vehicle-treated mice.
Lowered total caloric intake significantly on day 1 and throughout the study compared to vehicle-treated mice.
Reduced body weight change from day 0 significantly over the 11-day study compared to vehicle-treated mice.
Animal Model: C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed Clinton 40% high-fat diet)[1]
Dosage: 60 mg/kg/day
Administration: p.o.; continuous dietary admixture; 17 days
Result: Reduced hepatic triglyceride levels (measured as mg/liver and mg/g liver) significantly compared to vehicle-treated mice.
Animal Model: C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed 45% high-fat diet)[1]
Dosage: 60 mg/kg/day
Administration: p.o.; continuous dietary admixture; 3 weeks
Result: Reduced serum total cholesterol and serum triglyceride levels significantly compared to vehicle-treated mice.
Animal Model: C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed 45% high-fat diet for at least 13 weeks)[1]
Dosage: 60 mg/kg
Administration: p.o.; single pretreatment dose; 30 minutes before HFD meal
Result: Increased plasma active glucagon-like peptide-1 (aGLP-1) levels compared to vehicle treatment, with peak levels at 5-10 minutes after HFD meal.
Produced a synergistic increase in plasma aGLP-1 levels when combined with sitagliptin, with significantly higher levels at 5, 10, 15, 30, 60, 120, and 240 minutes after HFD meal compared to vehicle, sitagliptin alone, or LP-856866 alone.
Molecular Weight

521.55

Formula

C26H26F3NO5S
Appearance

Solid

Color

White to light yellow

SMILES

C[C@H](C1=CC=CC(OC2=CC=CC=C2)=C1)OC3=CC=C(C=C3C(F)(F)F)C(NS(=O)(C(C)(C)C)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9174 mL 9.5868 mL 19.1736 mL
5 mM 0.3835 mL 1.9174 mL 3.8347 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 1.9174 mL 9.5868 mL 19.1736 mL 47.9340 mL
5 mM 0.3835 mL 1.9174 mL 3.8347 mL 9.5868 mL
10 mM 0.1917 mL 0.9587 mL 1.9174 mL 4.7934 mL
15 mM 0.1278 mL 0.6391 mL 1.2782 mL 3.1956 mL
20 mM 0.0959 mL 0.4793 mL 0.9587 mL 2.3967 mL
25 mM 0.0767 mL 0.3835 mL 0.7669 mL 1.9174 mL
30 mM 0.0639 mL 0.3196 mL 0.6391 mL 1.5978 mL
40 mM 0.0479 mL 0.2397 mL 0.4793 mL 1.1984 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.9587 mL
60 mM 0.0320 mL 0.1598 mL 0.3196 mL 0.7989 mL
80 mM 0.0240 mL 0.1198 mL 0.2397 mL 0.5992 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.4793 mL
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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:

LP-856866LP856866LP 856866ACSL FamilyGLP ReceptorAcsl5 knockout micehuman ACSL5glucose homeostasisaGLP-1ileal brakehuman ACSL3ACSL1diet-induced obesityACSL5mouseInhibitorinhibitorinhibit

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