[CAS NO. 866405-64-3] Dorsomorphin

Name: Dorsomorphin
Brand: Arctom Scientific
SKU: AS080587

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PRODUCTS SPECIFICATIONS [866405-64-3]

Distributor

Catalog

AS080587

Brand

Arctom Scientific

CAS

866405-64-3

DESCRIPTION [866405-64-3]

Overview

MDL	MFCD08705402
Molecular Weight	399.49
Molecular Formula	C24H25N5O
SMILES	C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2

For research use only. We do not sell to patients.

321 Publications Citing Use of MCE

Summary

Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor ( K _i =109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2 , ALK3 , and ALK6 . Dorsomorphin induces autophagy ^[1] ^[2] .

IC50 & Target

AMPK

109 nM (Ki)

ACVR1

BMPR1A

ALK6

Autophagy

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] .

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] .

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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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°C)

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

H ₂ O : < 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
10 mM	0.2503 mL	1.2516 mL	2.5032 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: Saline

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

* All of the co-solvents are available by MCE.

References

Synonyms

Pyrazolo[1,5-a]pyrimidine, 6-[4-[2-(1-piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-

6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine

Dorsomorphin

Compound C

6-[4-(2-Piperidine-1-ylethoxy)phenyl]-3-pyridine-4-ylpyrazolo[1,5-a]pyrimidine