1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PPAR
  3. Seladelpar

Seladelpar  (Synonyms: MBX-8025)

目录号: HY-19522 纯度: 98.01%
COA 产品使用指南

Seladelpar (MBX-8025) 是一种有效的,具有口服活性的, 特异性 PPAR-δ 激动剂,EC50 为 2 nM。

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Seladelpar Chemical Structure

Seladelpar Chemical Structure

CAS No. : 851528-79-5

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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

生物活性

Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist[1][2].

IC50 & Target[1][2]

PPAR-δ

2 nM (EC50)

PPAR-α

1600 nM (EC50)

体外研究
(In Vitro)

Seladelpar (MBX-8025) is an orally active, potent (2 nM), and specific (>750-fold and >2500-fold compared with PPAR-α or PPAR-γ receptors, respectively) PPAR-δ agonist being developed as a lipid-altering agent[1]. Seladelpar is a potent, and selective PPAR-δ agonist (50% effect concentration human PPAR-δ=2 nM, PPAR-α=1,600 nM) that demonstrates favorable effects on insulin resistance, diabetes, and atherogenic dyslipidemia[2].

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

体内研究
(In Vivo)

From weaning, female Alms1 mutant (foz/foz) mice and wild-type littermates are fed an atherogenic diet for 16 weeks; groups (n=8-12) are then randomized to receive Seladelpar (10 mg/kg) or vehicle (1% methylcellulose) by gavage for 8 weeks. Despite minimally altering body weight, Seladelpar normalizes hyperglycemia, hyperinsulinemia, and glucose disposal in foz/foz mice. Serum alanine aminotransferase ranges 300-600 U/L in vehicle-treated foz/foz mice; Seladelpar reduces alanine aminotransferase by 50%. In addition, Seladelpar normalizes serum lipids and hepatic levels of free cholesterol and other lipotoxic lipids that are increased in vehicle-treated foz/foz versus wild-type mice. This abolished hepatocyte ballooning and apoptosis, substantially reduce steatosis and liver inflammation, and improve liver fibrosis. In vehicle-treated foz/foz mice, the mean nonalcoholic fatty liver disease activity score is 6.9, indicating nonalcoholic steatohepatitis (NASH); Seladelpar reverses NASH in all foz/foz mice (nonalcoholic fatty liver disease activity score 3.13). In atherogenic diet-fed Wt mice, administration of Seladelpar reduces body weight by ∼18% (P<0.05). In contrast, Seladelpar produces minimal effect on body weight in atherogenic diet–fed foz/foz mice. These animals develope severe hyperglycemia, hyperinsulinemia, and whole-body insulin resistance after 16 weeks (P<0.05); Seladelpar strikingly improves these indices (P<0.05). After intraperitoneal glucose injection, blood glucose reaches ~32 mM in vehicle-treated versus ~14 mM in Seladelpar-treated foz/foz mice (P<0.05); the area under the blood glucose disappearance curve is correspondingly lower in Seladelpar-treated foz/foz mice (P<0.05). Seladelpar produces a proportionally similar effect on glucose handling in atherogenic diet–fed Wt mice (P<0.05)[2].

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

Clinical Trial
分子量

444.46

Formula

C21H23F3O5S

CAS 号
性状

液体

颜色

Colorless to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (224.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2499 mL 11.2496 mL 22.4992 mL
5 mM 0.4500 mL 2.2499 mL 4.4998 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.62 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.62 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.75%

参考文献
Animal Administration
[2]

Mice[2]
From weaning (week 4), Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in both groups) are fed an atherogenic diet (23% fat, 0.2% cholesterol and 45% simple carbohydrate; 4.78 kcal/g digestible energy) ad libitum for 16 weeks, after which groups are randomized (n=8-12 mice/group) to once-a-day oral administration (by gavage) for 8 weeks of Seladelpar (10 mg/kg in 1% methylcellulose) or vehicle (controls). Animals are housed under 12-hour light/dark cycle and constant temperature of 22°C and receive maximal humane care[2].

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2499 mL 11.2496 mL 22.4992 mL 56.2480 mL
5 mM 0.4500 mL 2.2499 mL 4.4998 mL 11.2496 mL
10 mM 0.2250 mL 1.1250 mL 2.2499 mL 5.6248 mL
15 mM 0.1500 mL 0.7500 mL 1.4999 mL 3.7499 mL
20 mM 0.1125 mL 0.5625 mL 1.1250 mL 2.8124 mL
25 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2499 mL
30 mM 0.0750 mL 0.3750 mL 0.7500 mL 1.8749 mL
40 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4062 mL
50 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1250 mL
60 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9375 mL
80 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7031 mL
100 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5625 mL
Help & FAQs
  • 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.

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目录号:
HY-19522
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