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APD668

GPR119激动剂,APD668是GPR119激动剂，对人GPR119和大鼠GPR119的EC50分别为2.7 nM和33 nM。

目录号: PC10780 纯度: ≥98%

CAS No. :832714-46-2

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PC10780-5mg	5mg	¥1342.60	请登录
PC10780-10mg	10mg	¥2979.20	请登录
PC10780-50mg	50mg	¥9751.00	请登录
PC10780-100mg	100mg	¥16052.40	请登录
PC10780-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1568.00	请登录

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中文名称

APD668

中文别名

APD668 抑制剂;异丙基 4-(1-(2-氟-4-(甲基磺酰基)苯基)-1H-吡唑并[3,4-D]嘧啶-4-基氧基)哌啶-1-羧酸

英文名称

APD668

英文别名

1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester;1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl e;APD 668;Isopropyl 4-({1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3 ,4-d]pyrimidin-4-yl}oxy)-1-piperidinecarboxylate;ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE;APD-668

Cas No.

832714-46-2

分子式

C₂₁H₂₄N₅O₅FS

分子量

477.51

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC₅₀s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (K_i=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.

性状

Solid

IC50 & Target[1][2]

CYP2C9

0.1 μM (Ki)

hGPR119

2.7 nM (IC₅₀)

rGPR119

33 nM (IC₅₀)

hERG channel

3 μM (IC₅₀)

体外研究(In Vitro)

APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC₅₀ of 23 nM.
APD668 is highly bound to plasma proteins of male and female cynomolgus monkeys and humans (?99%), but is less extensively bound to male (93.0%) and female (96.6%) rats.

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

体内研究(In Vivo)

APD668 (10-30 mg/kg; p.o. once daily for 8 weeks) significantly reduces blood glucose and glycated hemoglobin (HbA1c) levels, with no desensitization of the acute drug response.
APD668 (1-10 mg/kg; a single p.o.) markedly reduces blood glucose levels during oral glucose tolerance test in a dose-dependent manner in mice.
APD668 (0.08 mg/kg/min; i.v.) shows no effect during euglycemic condition, but significantly stimulates insulin release when blood glucose levels are raised to approximately 300 mg/dl in a hyperglycemic clamp model in the Sprague-Dawley rat.
APD668 (p.o.) exhibits rapid to moderate absorption (t_max≤2 h) in mice, rats, and monkeys, but slower in dogs (t_max=6 h), and moderate to good absolute oral bioavailability (44-79%) in mice, rats, and monkeys, but lower in dogs (22%).

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

Animal Model:	Male Zucker Diabetic Fatty (ZDF) rats (6 weeks old, 200-250 g)
Dosage:	10, 30 mg/kg
Administration:	P.o. once daily for 8 weeks
Result:	Decreased the blood glucose and HbA1c levels at 30 mg/kg/day. Did not develop diabetes, whereas the vehicle treated rats did.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Semple G, et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. [Information]

[2]. Bahirat UA, et, al. APD668, a G protein-coupled receptor 119 agonist improves fat tolerance and attenuates fatty liver in high-trans fat diet induced steatohepatitis model in C57BL/6 mice. Eur J Pharmacol. 2017 Apr 15;801:35-45. [Information]

溶解度数据

体外研究:

DMSO : 33.33 mg/mL (69.80 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0942 mL	10.4710 mL	20.9420 mL
5 mM	0.4188 mL	2.0942 mL	4.1884 mL
10 mM	0.2094 mL	1.0471 mL	2.0942 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 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。
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.36 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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