1. Metabolic Enzyme/Protease
  2. Carnitine Palmitoyltransferase (CPT) Acyltransferase
  3. 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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Teglicar chloride

Teglicar chloride Chemical Structure

CAS No. : 908566-80-3

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Description

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[1].

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.

In Vivo

Teglicar (50 mg/kg; p.o.; twice daily; 45 days) chloride produces a 25% reduction in serum glucose levels and improves glucose homeostasis in male C57BL/KsJ-db/db mice without affecting cardiac parameters[1].
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.

Animal Model: C57BL/KsJ-db/db (male, 8 weeks old)[1]
Dosage: 50 mg/kg
Administration: p.o.; twice daily; 45 days
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.
Molecular Weight

436.07

Formula

C22H46ClN3O3

CAS No.
SMILES

CCCCCCCCCCCCCCNC(N[C@H](CC(O)=O)C[N+](C)(C)C)=O.[Cl-]

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Teglicar chloride
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HY-182248
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