Dorsomorphin [866405-64-3]

Katalog-Nummer HY-13418A-10mg

Size : 10mg

Marke : MedChemExpress


Beschreibung

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 can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599)[1][2].

IC50 & Target[1][2]

AMPK

109 nM (Ki)

ACVR1

 

BMPR1A

 

ALK6

 

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
A2780 EC50
0.9 μM
Compound: 1; Cpd C
Antimitotic activity against human A2780 cells by ATP lite luminescence assay
Antimitotic activity against human A2780 cells by ATP lite luminescence assay
[PMID: 31831383]
MCF7 EC50
4.9 μM
Compound: 1; Cpd C
Antimitotic activity against human MCF7 cells by ATP lite luminescence assay
Antimitotic activity against human MCF7 cells by ATP lite luminescence assay
[PMID: 31831383]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molekulargewicht

399.49

Formel

C24H25N5O

CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Lösungsmittel & Löslichkeit
In Vitro: 

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

DMSO : 25 mg/mL (62.58 mM; ultrasonic and adjust pH to 3 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (25.03 mM); Suspended solution; Need ultrasonic and warming and heat to 35°C

  • Protocol 2

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 10 mg/mL (25.03 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

Sie könnten auch an folgenden Produkten interessiert sein:



Katalog-Nummer
Beschreibung
Cond.
Preis zzgl. MwSt.
100-116-10UG
 10UG 
SY-PD0325901-1mg
 1 mg 
1801-SC
 500ml