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BML-275

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BML-275 Basic information

Product Name:
BML-275
Synonyms:
  • dorsoMorphin (Hydrochloride)
  • DorsoMorphin, Dihydrochloride Salt, >99%
  • BML-275,Compound C
  • 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine hydrochloride (1:2) Dorsomorphin 2HCl
  • Dorsomorphin-2HCl BML-275
  • 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)pyrazolo[1,5-a]pyrimidine hydrochloride (1:2)
  • BML-275 dihydrochloride
  • Dorsomorphin(BML-275)dihydrochloride
CAS:
1219168-18-9
MF:
C24H27Cl2N5O
MW:
472.41008
Product Categories:
  • PI3K/Akt/mTOR
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
Mol File:
1219168-18-9.mol
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BML-275 Chemical Properties

storage temp. 
under inert gas (nitrogen or Argon) at 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
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BML-275 Usage And Synthesis

Description

Dorsomorphin (hydrochloride) is a potent, reversible inhibitor of AMP kinase (AMPK; Ki = 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

BML-275Supplier

J & K SCIENTIFIC LTD.
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Jinan Trio PharmaTech Co., Ltd.
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0531-88811783
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sales@trio-pharmatech.com
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