AS1708727|cas:1253226-93-5|西域试剂

AS1708727,99.82%

产品编号：Bellancom-123046| CAS NO：1253226-93-5| 分子式：C₂₄H₂₄Cl₂N₂O₂| 分子量：443.37

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-123046	￥3000.00	杭州北京（现货）
Bellancom-123046	￥4800.00	杭州北京（现货）
Bellancom-123046	￥9500.00	杭州北京（现货）
Bellancom-123046	￥14500.00	杭州北京（现货）
Bellancom-123046	￥22500.00	杭州北京（现货）

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AS1708727

产品介绍

AS1708727 是口服有效的 Foxo1 抑制剂，其对 G6Pase 和 PEPCK 的 EC₅₀ 值分别为 0.33 μM 和0.59 μM。

生物活性

AS1708727 is an orally active Foxo1 inhibitor, with EC₅₀ values of 0.33 μM and 0.59 μM for G6Pase and PEPCK, respectively.

体外研究

AS1708727 suppresses increases in blood glucose level by inhibiting gluconeogenic gene expression.

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

RT-PCR

Cell Line:	Fao cells, derived from the H4IIE hepatoma cell line.
Concentration:	0.1-3000 μM.
Incubation Time:	18 h.
Result:	Showed dose-dependent reduction in mRNA levels for G6Pase and PEPCK.

体内研究
(In Vivo)

AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects.

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

Animal Model:	db/db mice aged six weeks.
Dosage:	100-1000 mg/kg (Pharmacokinetic Analysis).
Administration:	Orally.
Result:	C_max) was 26.7 μM and maximum drug concentration time (T_max) of 0.5 h at 300 mg/kg. Liver concentration of AS1708727 at 0.5-2 h after oral administration was 3.7- to 5.4-fold higher than the plasma concentration, indicating good liver transition of AS1708727.

Animal Model:	Diabetic model mice.
Dosage:	30 to 300 mg/kg.
Administration:	Orally twice daily for 4 days.
Result:	Blood glucose level was significantly reduced at 300 mg/kg. Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg. G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg.

体内研究

AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects.

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

Animal Model:	db/db mice aged six weeks.
Dosage:	100-1000 mg/kg (Pharmacokinetic Analysis).
Administration:	Orally.
Result:	C_max) was 26.7 μM and maximum drug concentration time (T_max) of 0.5 h at 300 mg/kg. Liver concentration of AS1708727 at 0.5-2 h after oral administration was 3.7- to 5.4-fold higher than the plasma concentration, indicating good liver transition of AS1708727.

Animal Model:	Diabetic model mice.
Dosage:	30 to 300 mg/kg.
Administration:	Orally twice daily for 4 days.
Result:	Blood glucose level was significantly reduced at 300 mg/kg. Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg. G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg.

体内研究

AS1708727 (30 to 300 mg/kg, orally) reduces both blood glucose and triglyceride levels, exhibiting anti-diabetic effects.

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

Animal Model:	db/db mice aged six weeks.
Dosage:	100-1000 mg/kg (Pharmacokinetic Analysis).
Administration:	Orally.
Result:	C_max) was 26.7 μM and maximum drug concentration time (T_max) of 0.5 h at 300 mg/kg. Liver concentration of AS1708727 at 0.5-2 h after oral administration was 3.7- to 5.4-fold higher than the plasma concentration, indicating good liver transition of AS1708727.

Animal Model:	Diabetic model mice.
Dosage:	30 to 300 mg/kg.
Administration:	Orally twice daily for 4 days.
Result:	Blood glucose level was significantly reduced at 300 mg/kg. Plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were significantly reduced at 300 mg/kg. G6Pase and PEPCK mRNA levels were significantly reduced at dosages of 100 and 300 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (93.98 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2555 mL	11.2773 mL	22.5545 mL
5 mM	0.4511 mL	2.2555 mL	4.5109 mL
10 mM	0.2255 mL	1.1277 mL	2.2555 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°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。

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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.69 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.69 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.69 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.69 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。