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Dorsomorphin
本半岛bd体育手机客户端 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

半岛bd体育手机客户端 名称
Compound C
BML-275
半岛bd体育手机客户端 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 ALK2， ALK3和 ALK6。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 mg 5 mg 10 mg
1 mM 2.5032 mL 12.5160 mL 25.0319 mL
5 mM 0.5006 mL 2.5032 mL 5.0064 mL
10 mM 0.2503 mL 1.2516 mL 2.5032 mL
*

请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 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。
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