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Dorsomorphin
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。
Dorsomorphin图片
CAS NO:866405-64-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
Compound C
BML-275
产品介绍
Dorsomorphin (Compound C) 是一种选择性,ATP 竞争性的AMPK抑制剂 (在没有 AMP 的情况下,Ki为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体ALK2ALK3ALK6。Dorsomorphin 诱导自噬 (autophagy) 作用。
生物活性

Dorsomorphin (Compound C) is a selective and ATP-competitiveAMPKinhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptorsALK2,ALK3, andALK6. Dorsomorphin inducesautophagy[1][2].

IC50& Target[1][2]

AMPK

109 nM (Ki)

ACVR1

 

BMPR1A

 

ALK6

 

Autophagy

 

体外研究
(In Vitro)

Dorsomorphin (compound C) (0-10 μM, 18 h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells[2].

Western Blot Analysis[2]

Cell Line:Human fibrosarcoma HT1080 cells
Concentration:0-10 μM.
Incubation Time:18 hours.
Result:Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner and also suppressed GRP78 promoter activity induced by glucose withdrawal.
体内研究
(In Vivo)

Dorsomorphin (compound C: 10 mg/kg, intravenously once) treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increasing serum iron concentrations in adult mice[3].
Dorsomorphin (compound C: 0.2 mg/kg, I.V., 30 min before LPS injection) reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta[4].
Dorsomorphin (compound C; 25 mg/kg; i.p. injection; in male BALB/c mice) treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only[5].

Animal Model:Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin[3].
Dosage:10 mg/kg.
Administration:Intravenously once.
Result:Led to a 60% increase in total serum iron concentrations.
Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice.
Animal Model:Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250 g)[4].
Dosage:0.2 mg/kg.
Administration:I.V., 30 min before LPS injection.
Result:Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.
Animal Model:Male BALB/c mice at 6-7 weeks of age weighing 20-22 g[5]
Dosage:25 mg/kg
Administration:Injection i.p.; 60 min before LPS challenge
Result:Treatment of mice with 25 mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only.
分子量

399.49

性状

Solid

Formula

C24H25N5O

CAS 号

866405-64-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

1M HCl : 50 mg/mL(125.16 mM;ultrasonic and adjust pH to 1 with HCl)

DMSO : 5 mg/mL(12.52 mM;ultrasonic and warming and heat to 80℃)

Ethanol : 3.33 mg/mL(8.34 mM;Need ultrasonic)

H2O :< 0.1 mg/mL(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5032 mL12.5160 mL25.0319 mL
5 mM0.5006 mL2.5032 mL5.0064 mL
10 mM0.2503 mL1.2516 mL2.5032 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 (protect from light)。-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: Saline

    Solubility: 12.5 mg/mL (31.29 mM); Clear solution; Need ultrasonic and adjust pH to 5 with 0.1 M HCL

*以上所有助溶剂都可在本网站选购。