BML-275,Compound C; BML275; BML-275; BML 275; CpdC;Dorsomorphin
Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Targets |
AMPK (Ki = 109 nM); ACVR1; BMPR1A; ALK6; Autophagy
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ln Vitro |
Dorsomorphin reduces the ability of AICAR and metformin to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes, as well as their ability to inactivate ACC. [1]
In HT-29 cells, Dorsomorphin almost entirely prevents autophagic proteolysis by inhibiting AMPK activity.[2] Dorsomorphin additionally blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription, and osteogenic differentiation by selectively inhibiting the BMP type I receptors ALK2, ALK3 and ALK6.[3] |
ln Vivo |
Dorsomorphin (10 mg/kg) increases serum iron levels and lowers basal levels of hepcidin expression in adult mice. [3]
Dorsomorphin (0.2 mg/kg, i.v.) significantly lowers VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4] |
Enzyme Assay |
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPKinhibitor, with aKiof 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3 and ALK6.
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Cell Assay |
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.
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Animal Protocol |
Iron-replete mice; Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.
10 mg/kg. Intravenously once. 12-week-old C57BL/6 mice raised on a standard diet are injected via the tail vein with 0.2 g/kg of Dextran or 0.2 g/kg of iron-dextran USP. Dextran is injected with vehicle only, whereas iron-dextran is injected with either vehicle or Dorsomorphin (10 mg/kg). 1 h after injection, mice are killed and liver segments are collected in 500 µL of SDS-lysis buffer and mechanically homogenized. 20 µL of liver extracts are resolved by SDS-PAGE and immunoblotted. Total RNA is harvested using Trizol from mechanically homogenized mouse livers (6 h after injection with a single intraperitoneal dose of Dorsomorphin (10 mg/kg) or DMSO).[3] |
References |
Molecular Formula |
C24H25N5O
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Molecular Weight |
399.49
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Exact Mass |
399.2059
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Elemental Analysis |
C, 72.16; H, 6.31; N, 17.53; O, 4.00
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CAS # |
866405-64-3
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Related CAS # |
Dorsomorphin dihydrochloride;1219168-18-9;Dorsomorphin dihydrochloride;1219168-18-9
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Appearance |
Light yellow to yellow solid powder
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LogP |
2.39
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tPSA |
55.55
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SMILES |
C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2
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InChi Key |
XHBVYDAKJHETMP-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2
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Chemical Name |
6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~3 mg/mL (7.5 mM)
Water: <1 mg/mL Ethanol: 2 mg/mL (5.0 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (25.03 mM) in 50% PEG300 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 10 mg/mL (25.03 mM) in 0.5% CMC/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.