Dorsomorphin (Synonyms:Compound C; BML-275)
目录号 : KM10457 CAS No. : 866405-64-3 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
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10mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.

体外研究

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.

Western Blot Analysis

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

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.
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.
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.

Animal Model: Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.
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).
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
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.
分子式
C24H25N5O
分子量
399.49
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 中的溶解度 : 50 mg/mL (125.16 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

DMSO 中的溶解度 : 33.33 mg/mL (83.43 mM; ultrasonic and adjust pH to 2 with 1M HCl; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 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 (protect from light)。-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: 0.5% CMC-Na/saline water

    Solubility: 26 mg/mL (65.08 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 3.3 mg/mL 的澄清 EtOH 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。

  • 3.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 3.3 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 0.33 mg/mL (0.83 mM); Clear solution

    此方案可获得 ≥ 0.33 mg/mL (0.83 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 3.3 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 5.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 2.0 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。

  • 6.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 2.0 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。

  • 7.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 0.2 mg/mL (0.50 mM); Clear solution

    此方案可获得 ≥ 0.2 mg/mL (0.50 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 2.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献

纯度: 98%

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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