2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. Teglicar chloride

Teglicar chloride (ST1326 chloride) 是一种具有口服活性的、可逆的、混合型的、选择性的肝脏肉碱棕榈酰转移酶 I (L-CPT I) 抑制剂，其对大鼠 L-CPT I 的 IC50 为 1.1 μM。Teglicar chloride 可降低血清葡萄糖水平。Teglicar chloride 在正常禁食大鼠中显示出抗酮症活性。Teglicar chloride 可用于 2 型糖尿病、酮症酸中毒的相关研究。

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Teglicar chloride

Teglicar chloride Chemical Structure

CAS No. : 908566-80-3

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Teglicar chloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

L-CPT I

1.1 μM (IC50)

体外研究
(In Vitro)

Teglicar chloride (0-3 mM; 1 min) 可强效且选择性地抑制大鼠肝线粒体中的肉碱棕榈酰转移酶 I 肝亚型 (L-CPT I)，其 IC50 为 1.1 μM；对大鼠心脏线粒体中的肉碱棕榈酰转移酶 I 心脏亚型 (M-CPT I) 的抑制效力低 39.4 倍，IC50 为 43.4 μM[1]。
Teglicar chloride (最高 50 μM；48 h) 在大鼠肝细胞中无细胞毒性[1]。
Teglicar chloride (0.5-1.0 μM) 是毕赤酵母 (Pichia pastoris) 中表达的 L-CPT I 的可逆性混合型抑制剂 (以棕榈酰辅酶 A 为参照)，其表观 Ki 为 0.36 ± 0.04 μM[1]。

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

Teglicar chloride 相关抗体:
体内研究
(In Vivo)

Teglicar chloride (50 mg/kg；口服；每日 2 次；连续 45 天) 可使雄性 C57BL/KsJ-db/db 小鼠的血清葡萄糖水平降低 25%，并改善其葡萄糖稳态，且不会影响心脏相关参数[1]。
Teglicar chloride (10-40 mg/kg；口服) 可使禁食 24 小时的雄性 Sprague Dawley 大鼠血清 β-hydroxybutyrate 水平呈剂量依赖性降低，其 ED50 为 14.5 mg/kg[1]。

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.
分子量

436.07

Formula

C22H46ClN3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Teglicar chloride 相关分类

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  • 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:

Teglicar908566-80-3ST1326ST 1326ST-1326AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseketoacidosisSprague Dawley ratsliver carnitine palmitoyltransferase IC57BL/KsJ-db/db micetype ii diabetes mellitusL-CPT Irat hepatocytesPichia pastorisrat liver mitochondriarat heart mitochondriaInhibitorinhibitorinhibit

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