| Identification | Back Directory | [Name]
BAY 41-2272 | [CAS]
256376-24-6 | [Synonyms]
IN1523
UNII-34A162J6WB
3-(4-Amino-5-cyclopropylpyrimidin-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3
5-Cyclopropyl-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-4-amine
5-Cyclopropyl-2-[1-[(2-fluorophenyl)Methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-pyriMidinaMine
4-Pyrimidinamine, 5-cyclopropyl-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-
BAY 41-2272; 256376-24-6; UNII-34A162J6WB; IN1523; BAY-41-2272; 3-(4-AMINO-5-CYCLOPROPYLPYRIMIDIN-2-YL)-1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3;4-B]PYRIDINE | [Molecular Formula]
C20H17FN6 | [MDL Number]
MFCD06411391 | [MOL File]
256376-24-6.mol | [Molecular Weight]
360.39 |
| Chemical Properties | Back Directory | [Melting point ]
210.5-211.4 °C
| [Boiling point ]
496.1±45.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
DMSO: 26 mg/mL at 60 °C
| [form ]
solid
| [pka]
2.71±0.10(Predicted) | [color ]
white
|
| Hazard Information | Back Directory | [Description]
Soluble guanylate cyclase (sGC), a receptor for nitric oxide (NO), is a heterodimer consisting of alpha and beta subunits, with the beta subunit featuring a heme-nitric oxide (H-NOX) binding domain. The binding of NO to H-NOX induces sGC to generate the second messenger cGMP. BAY 41-2272 is a pyrazolopyridine compound that acts as an activator of sGC, stimulating activity to a level that would be expected to cause biologically important increases in cGMP at concentrations as low as 10-100 nM. Through this effect, it inhibits platelet aggregation (IC50 = 36 nM), induces relaxation of phenylephrine-preconstricted rabbit aorta rings (IC50 = 304 nM), and reduces proliferation in smooth muscle. BAY 41-2272 is effective in vivo, as it decreases mean arterial blood pressure in hypertensive rats. Unlike another sGC activator, YC-1 , BAY 41-2772 does not inhibit phosphodiesterases. | [Uses]
BAY 41-2272 is a soluble guanylate cyclase agonist that activates human mononuclear phagocytes. Inhibits vascular smooth muscle growth through the cAMP-dependent protein kinase and cGMP-dependent protein kinase pathways. | [Definition]
ChEBI: BAY 41-2272 is a pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted by a 2-fluorobenzyl group at position 1 and by a 4-amino-5-cyclopropylpyrimidin-2-yl group at position 3. It is an activator of soluble guanylate cyclase. It has a role as a soluble guanylate cyclase activator, a platelet aggregation inhibitor, a vasodilator agent and an antihypertensive agent. It is a pyrazolopyridine, a member of monofluorobenzenes, an aminopyrimidine and a member of cyclopropanes. | [General Description]
A cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 μM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α1 and α2 subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC50 = 304 nM) and blocks collagen-induced aggregation of human platelets (IC50 = 36 nM). Does not inhibit phosphodiesterases. | [Biochem/physiol Actions]
Cell permeable: yes | [storage]
Store at +4°C |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
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