APD668

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APD668

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

832714-46-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

APD668 是一种有效的，选择性和具有口服活性的 G 蛋白偶联受体GPR119激动剂，对hGPR119和rGPR119的EC₅₀值分别为 2.7 nM 和 33 nM。APD668 对除CYP2C9(K_i=0.1 μM) 以外的五种主要 CYP 亚型均无明显抑制作用。APD668 可用于脂肪性肝炎和糖尿病的研究。

生物活性

APD668 is a potent, selective and orally active agonist ofG-protein coupled receptorGPR119, withEC₅₀s of 2.7 nM and 33 nM forhGPR119andrGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception ofCYP2C9(K_i=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes^[1]^[2].

IC₅₀& Target

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 EC₅₀of 23 nM^[1].
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^[1].

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^[1].
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^[1].
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^[1].
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%)^[1].

Animal Model:	Male Zucker Diabetic Fatty (ZDF) rats (6 weeks old, 200-250 g)^[1]
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.

分子量

477.51

性状

Solid

Formula

C₂₁H₂₄FN₅O₅S

CAS 号

832714-46-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

配制储备液

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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

1.
请依序添加每种溶剂： 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.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 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

*以上所有助溶剂都可在本网站选购。