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
- Formule: C22H46ClN3O3
- Masse moléculaire:436.07
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CPT-1 |
L-CPT I 1.1 μM (IC50) |
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.
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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Masse moléculaire 436.07
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Teglicar chloride Related Classifications
HY-182248 Related Classifications
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- 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