Teglicar chloride
Teglicar chloride (ST1326 chloride) is an orally active, reversible, mixed-type, selective inhibitor of hepatic carnitine palmitoyltransferase I (L-CPT I), with an IC50 of 1.1 μM against rat L-CPT I. Teglicar chloride reduces serum glucose levels. Teglicar chloride exhibits antiketotic activity in normal fasted rats. Teglicar chloride can be used in research related to type 2 diabetes and ketoacidosis.
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- CAS No.: 908566-80-3
- 화학식: C22H46ClN3O3
- 분자량:436.07
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[1]|
CPT-1 |
L-CPT I 1.1 μM (IC50) |
In Vitro
Teglicar (0-3 mM; 1 min) chloride potently and selectively inhibits liver isoform CPT I (L-CPT I) from rat liver mitochondria with an IC50 of 1.1 μM, and shows 39.4-fold lower potency against heart isoform CPT I (M-CPT I) from rat heart mitochondria with an IC50 of 43.4 μM[1].
Teglicar (up to 50 μM; 48 h) chloride shows no cytotoxicity in rat hepatocytes at concentrations up to 50 μM after 48 h of incubation[1].
Teglicar (0.5-1.0 μM) chloride acts as a reversible, mixed inhibitor of L-CPT I expressed in Pichia pastoris with respect to palmitoyl-CoA, exhibiting an apparent Ki of 0.36 ± 0.04 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Teglicar (10-40 mg/kg; p.o.) chloride produces a dose-dependent reduction in serum β-hydroxybutyrate levels in 24-hour fasted male Sprague Dawley rats, with an ED50 of 14.5 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/KsJ-db/db (male, 8 weeks old)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily; 45 days
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Result:Reduced serum glucose levels by 25% (from 673.9 ± 44.09 mg/dL to 506.6 ± 59.12 mg/dL).
Reduced serum fructosamine levels by 30% (from 4.80 ± 0.17 mmol/L to 3.36 ± 0.30 mmol/L).
Reduced liver glycogen by 25%.
Increased liver triglyceride content by 38%.
Increased serum free fatty acid levels by 20%.
Caused no significant changes in serum insulin, leptin, triglyceride, urea, alanine aminotransferase, or cholesterol levels.
Caused no effects on heart weight or heart triglyceride content.
Chemical Information
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CAS No. 908566-80-3
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분자량 436.07
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화학식 C22H46ClN3O3
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SMILES
CCCCCCCCCCCCCCNC(N[C@H](CC(O)=O)C[N+](C)(C)C)=O.[Cl-]
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Synonyms
ST1326 chloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Teglicar
- 908566-80-3
- ST1326
- ST 1326
- ST-1326
- Carnitine Palmitoyltransferase (CPT)
- Acyltransferase
- ketoacidosis
- Sprague Dawley rats
- liver carnitine palmitoyltransferase I
- C57BL/KsJ-db/db mice
- type ii diabetes mellitus
- L-CPT I
- rat hepatocytes
- Pichia pastoris
- rat liver mitochondria
- rat heart mitochondria
- Inhibitor
- inhibitor
- inhibit