LP-856866
Based on 1 Customer Validation
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.92%
- 화학식: C26H26F3NO5S
- 분자량:521.55
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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ACSL5 |
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.
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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]
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Dosage:10 mg/kg/day; 30 mg/kg/day; 60 mg/kg/day
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Administration:p.o.; continuous dietary admixture; 28 days
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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.
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Animal Model:C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; chow-fed, acclimated to 10% low-fat diet for 2 weeks)[1]
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Dosage:75 mg/kg/day
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Administration:p.o.; continuous dietary admixture; 11 days
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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.
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Animal Model:C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed Clinton 40% high-fat diet)[1]
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Dosage:60 mg/kg/day
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Administration:p.o.; continuous dietary admixture; 17 days
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Result:Reduced hepatic triglyceride levels (measured as mg/liver and mg/g liver) significantly compared to vehicle-treated mice.
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Animal Model:C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed 45% high-fat diet)[1]
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Dosage:60 mg/kg/day
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Administration:p.o.; continuous dietary admixture; 3 weeks
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Result:Reduced serum total cholesterol and serum triglyceride levels significantly compared to vehicle-treated mice.
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Animal Model:C57BL/6J-Tyrc−Brd X 129SvEvBrd hybrid (male; fed 45% high-fat diet for at least 13 weeks)[1]
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Dosage:60 mg/kg
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Administration:p.o.; single pretreatment dose; 30 minutes before HFD meal
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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.
Chemical Information
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Appearance Solid
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분자량 521.55
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화학식 C26H26F3NO5S
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Color White to light yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
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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