BC1618

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BC1618

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:

2222094-18-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

BC1618，是具有口服活性的Fbxo48抑制剂，可刺激 Ampk 信号 (阻止激活的 pAmpkα 被 Fbxo48 介导的蛋白酶体降解)。BC1618 促进线粒体分裂、促进自噬，提高肝脏胰岛素的敏感性。

生物活性

BC1618, an orally activeFbxo48inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitatesautophagyand improves hepaticinsulinsensitivity^[1].

体外研究
(In Vitro)

BC1618 enhances pAmpkα protein stability during CHX treatment^[1].
BC1618 displays more than 1,000-fold enhanced activity to stimulate pAmpkα in cells than metformin^[1].
BC1618 (0.1-2 μM, 16 h) induced dose- and time-dependent increases in pAmpkα and pACC protein levels are also confirmed in human primary-like hepatocytes^[1].
BC1618 (1 μM) effectively disrupts the interaction between Fbxo48 and pAmpkα, and has no effect on Fbxo48, Ampkα1 or Ampkα2 messenger RNAs^[1].
BC1618 increases the abundance of a series of autophagic marker proteins during glucose depletion. BC1618 induces phosphorylation of the mTORC1 associated protein Raptor, reducing pS6 levels, all consistent with the known mTOR inhibitory effects exerted by activated Ampk^[1].

Western Blot Analysis^[1]

Cell Line:	BEAS-2B cells.
Concentration:	0-2 μM.
Incubation Time:	16 h.
Result:	Induced pAmpkα and pACC protein levels dose-dependently.

体内研究
(In Vivo)

BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity in high-fat-diet-induced obese mice^[1].
BC1618, appears to be ~1,000-fold more potent than metformin and is extremely well tolerated in mice^[1].
BC1618 displays excellent oral bioavailability with a peak of 2,000 ng/mL within 0.5h and 500 ng/mL in plasma at 4h after an oral load of 20mg/kg^[1].

Animal Model:	C57BL/6 mice^[1].
Dosage:	2 or 10 mg/kg (challenged with LPS (3 mg/kg) for an additional 18 h).
Administration:	IP, once.
Result:	Reduced lung inflammation in endotoxin treated mice.

Animal Model:	C57BL/6 mice^[1].
Dosage:	15 and 30 mg/kg/d.
Administration:	Drinking water for 3 months.
Result:	Exhibited no obvious toxicity.

分子量

415.45

性状

Solid

Formula

C₂₄H₂₄F₃NO₂

CAS 号

2222094-18-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL(240.70 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4070 mL	12.0351 mL	24.0703 mL
5 mM	0.4814 mL	2.4070 mL	4.8141 mL
10 mM	0.2407 mL	1.2035 mL	2.4070 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： 50%PEG300 50% saline
Solubility: 5 mg/mL (12.04 mM); Suspended solution; Need ultrasonic
2.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: 2.5 mg/mL (6.02 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.02 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 25.0 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
3.
请依序添加每种溶剂： 10% DMSO 90%corn oil
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.02 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。

*以上所有助溶剂都可在本网站选购。