Arhalofenate (Synonyms: 芳卤芬酯; MBX 102; JNJ 39659100)

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Arhalofenate (MBX 102) 是选择性的(PPAR)-γ部分激动剂，常用于 2 型糖尿病的研究。

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Arhalofenate Chemical Structure

CAS No. : 24136-23-0

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MCE 顾客使用本产品发表的 1 篇科研文献

•Drug Dev Res. 2020 Nov;81(7):859-866. [Abstract]

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PPARα PPARβ/δ PPARγ PPAR PPARδ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

IC₅₀ & Target

PPAR-γ

体外研究
(In Vitro)

Arhalofenate (MBX 102) is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. Arhalofenate (MBX 102) shows a dose-dependent activation of mouse GAL4-PPAR-γ with EC₅₀s of appr 12 μM^[2].

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

体内研究
(In Vivo)

Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (MBX 102) (60 mg/kg) leads to a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels^[1]. Arhalofenate (MBX 102) (100 mg/kg, p.o.) significantly decreases triglyceride, free fatty acid, and cholesterol levels in ZDF rats. MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (MBX 102) (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats^[2].

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

Clinical Trial

分子量

415.79

Formula

C₁₉H₁₇ClF₃NO₄

CAS 号

24136-23-0

中文名称

芳卤芬酯

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

产品使用指南 (1538 KB)

参考文献

[1]. Gregoire FM, et al. MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88. [Content Brief]

[2]. Chandalia A, et al. MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activation. PPAR Res. 2009;2009:706852. [Content Brief]

Animal Administration ^[1]	Male ZDF rats at 8 wk of age are used in the assay. ZDF rats are single housed and allowed access ad libitum to tap water and chow. ZDF rats are screened into three groups with similar mean plasma glucose levels. ZDF rats are cannulated in the jugular vein and the carotid artery and are allowed to recover at least for 2 d. Rats are dosed with either vehicle or Arhalofenate (MBX 102) (100 mg/kg) by oral gavage for 4-7 d. On the day of the clamp experiment, rats are dosed and food is withdrawn 1 h later. After rats are fasted for 4 h, blood samples are taken from the carotid catheter to measure basal glucose and insulin levels. Experiments are initiated with a priming injection (0.5 mL/rat of 5 μCi/mL of d-[3-³H] glucose) and initiation of a constant infusion of d-[3-³H] glucose tracer (8 μCi/mL) at a rate of 10 μL/min for 60 min. After the 1-h tracer-equilibration period, a post-tracer blood sample is collected for glucose, insulin and d-[3-³H] glucose specific activity (SA) measurements. Infusion of tracer glucose is then discontinued, and insulin infusion is initiated (10 μL/min equivalent to 40 mU/kg/min) along with glucose infusion. The glucose infusion rate is adjusted empirically to achieve plasma glucose level at 150 mg/dL ± 5% within the next 1.5-2 h. To facilitate this process, blood samples are collected at 10-min intervals for immediate plasma glucose measurements using a glucometer until the end of the study. Clamp is defined by three consecutive glucose measurements that are within the above defined range. Samples (300-400 μL) at the three time points (10-min interval) are collected for glucose, insulin, and d-[3-³H] glucose SA measurements. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Gregoire FM, et al. MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88. [Content Brief] [2]. Chandalia A, et al. MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activation. PPAR Res. 2009;2009:706852. [Content Brief]

Animal Administration
^[1]

Male ZDF rats at 8 wk of age are used in the assay. ZDF rats are single housed and allowed access ad libitum to tap water and chow. ZDF rats are screened into three groups with similar mean plasma glucose levels. ZDF rats are cannulated in the jugular vein and the carotid artery and are allowed to recover at least for 2 d. Rats are dosed with either vehicle or Arhalofenate (MBX 102) (100 mg/kg) by oral gavage for 4-7 d. On the day of the clamp experiment, rats are dosed and food is withdrawn 1 h later. After rats are fasted for 4 h, blood samples are taken from the carotid catheter to measure basal glucose and insulin levels. Experiments are initiated with a priming injection (0.5 mL/rat of 5 μCi/mL of d-[3-³H] glucose) and initiation of a constant infusion of d-[3-³H] glucose tracer (8 μCi/mL) at a rate of 10 μL/min for 60 min. After the 1-h tracer-equilibration period, a post-tracer blood sample is collected for glucose, insulin and d-[3-³H] glucose specific activity (SA) measurements. Infusion of tracer glucose is then discontinued, and insulin infusion is initiated (10 μL/min equivalent to 40 mU/kg/min) along with glucose infusion. The glucose infusion rate is adjusted empirically to achieve plasma glucose level at 150 mg/dL ± 5% within the next 1.5-2 h. To facilitate this process, blood samples are collected at 10-min intervals for immediate plasma glucose measurements using a glucometer until the end of the study. Clamp is defined by three consecutive glucose measurements that are within the above defined range. Samples (300-400 μL) at the three time points (10-min interval) are collected for glucose, insulin, and d-[3-³H] glucose SA measurements.

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

参考文献

[1]. Gregoire FM, et al. MBX-102/JNJ39659100, a novel peroxisome proliferator-activated receptor-ligand with weak transactivation activity retains antidiabetic properties in the absence of weight gain and edema. Mol Endocrinol. 2009 Jul;23(7):975-88. [Content Brief]

[2]. Chandalia A, et al. MBX-102/JNJ39659100, a novel non-TZD selective partial PPAR-γ agonist lowers triglyceride independently of PPAR-α activation. PPAR Res. 2009;2009:706852. [Content Brief]

Arhalofenate 相关分类

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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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:

Arhalofenate24136-23-0MBX 102 JNJ 39659100芳卤芬酯MBX102MBX-102JNJ39659100JNJ 39659100JNJ-39659100PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Arhalofenate (Synonyms: 芳卤芬酯; MBX 102; JNJ 39659100)

Arhalofenate 相关抗体

MCE 顾客使用本产品发表的 1 篇科研文献

Arhalofenate 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 PPAR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Arhalofenate 相关抗体:

Arhalofenate 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

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