ChemicalBook CAS DataBase List 1219168-18-9

1219168-18-9

Name	BML-275
CAS	1219168-18-9
Molecular Formula	C24H27Cl2N5O
MDL Number	MFCD11112197
Molecular Weight	472.41
MOL File	1219168-18-9.mol

Synonyms

CS-1883 Dorsomorph BML-275(2HCL) Compound C 2HCl Dorsomorphin HCl BML-275,Compound C BML-275 dihydrochloride Dorsomorphin-2HCl BML-275 BML-275 Dorsomorphin 2HCL Compound C dihydrochloride dorsoMorphin (Hydrochloride) DORSOMORPHIN (COMPOUND C) 2HCL Dorsomorphin 2HCl (BML-275 2HCl) BML-275; COMPOUND C; BML275; BML 275 Dorsomorphin(BML-275)dihydrochloride DORSOMORPHIN 2HCL;BML275.HCL;COMPOUND C DorsoMorphin, Dihydrochloride Salt, >99% Dorsomorphin (Compound C) dihydrochloride 6-[4-(2-PIPERIDIN-1-YLETHOXY)PHENYL]-3-PYRIDIN-4-YLPYRAZOLO[1,5-A]PYRIMIDINE;DIHYDROCHLORIDE 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine hydrochloride (1:2) BML-275;COMPOUND C;BML275;BML 275;BML-275 DIHYDROCHLORIDE;COMPOUND C DIHYDROCHLORIDE;BML275 DIHYDROCHLORIDE;BML 275 DIHYDROCHLORIDE 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine hydrochloride (1:2) Dorsomorphin 2HCl

Chemical Properties

storage temp.	Inert atmosphere,2-8°C
solubility	insoluble in EtOH; insoluble in H2O; ≥11.34 mg/mL in 0.9% NS ; ≥39.93 mg/mL in DMSO:H2O=2:1 ; ≥5.91 mg/mL in DMSO
form	Light yellow powder solid.
color	Yellow
Stability:	Hygroscopic

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501

Hazard Information

Description

Dorsomorphin (hydrochloride) is a potent, reversible inhibitor of AMP kinase (AMPK; K_i = 109 nM) that does not exhibit significant activity on structurally related kinases, including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin can also dose-dependently inhibit the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK6). Independent of AMPK inhibition, dorsomorphin, at 10 μM, has additionally been shown to downregulate the Akt/mTOR pathway to induce autophagy in U251 human glioma cells.

Uses

Dorsomorphin is an AMP-activated kinase (AMPK) inhibitor. Dorsomorphin selectively inhibits the bone morphogenetic protein (BMP) type I receptors ALK2, ALK3 and ALK6 and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. Dorsomorphin has shown to increase cisplatin-induced apoptosis, which was associated with hyper-induction of the tumor suppressor p53.

in vivo

Dorsomorphin (compound C; 10 mg/kg, intravenously once) dihydrochloride treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice^[3].
Dorsomorphin (0.2 mg/kg, i.v., 30 min before LPS injection) dihydrochloride reduces ICAM-1 and VCAM-1 expression in LPS-injected rat aorta^[4].
Dorsomorphin (25 mg/kg; i.p. injection, in male BALB/c mice) dihydrochloride 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.

IC 50

AMPK: 109 nM (Ki); ACVR1; BMPR1A; ALK6; Autophagy

storage

Room temperature (desiccate)

References

[1] ZHOU G, MYERS R W, LI Y, et al. Role of AMP-activated protein kinase in mechanism of metformin action.[J]. The Journal of clinical investigation, 2001, 1 1: 0. DOI: 10.1172/jci13505
[2] PAUL B YU. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism[J]. Nature chemical biology, 2007, 4 1: 33-41. DOI: 10.1038/nchembio.2007.54
[3] LJUBICA VUCICEVIC. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway.[J]. Autophagy, 2011, 7 1: 40-50. DOI: 10.4161/auto.7.1.13883

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