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| | BIX-02565 Basic information |
| Product Name: | BIX-02565 | | Synonyms: | BIX-02565;(5R)-N-[1-[3-(Dimethylamino)propyl]-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-5-methyl-1-oxo-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;CS-2569;BIX-02565;BIX02565;Inhibitor,BIX02565,BIX-02565,Ribosomal S6 Kinase (RSK),S6K,BIX 02565,inhibit;1H-[1,4]Diazepino[1,2-a]indole-8-carboxamide, N-[1-[3-(dimethylamino)propyl]-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-5-methyl-1-oxo-, (5R)-;(R)-N-(1-(3-(Dimethylamino)propyl)-1H-benzo[d]imidazol-2-yl)-5-methyl-1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;(5R)-N-{1-[3-(dimethylamino)propyl]-1H-1,3-benzodiazol-2-yl}-5-methyl-1-oxo-1H,2H,3H,4H,5H-[1,4]diazepino[1,2-a]indole-8-carboxamide | | CAS: | 1311367-27-7 | | MF: | C26H30N6O2 | | MW: | 458.56 | | EINECS: | | | Product Categories: | | | Mol File: | 1311367-27-7.mol |  |
| | BIX-02565 Chemical Properties |
| density | 1.32±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥22.95 mg/mL in DMSO; insoluble in H2O; ≥3.17 mg/mL in EtOH with gentle warming and ultrasonic | | form | Powder | | pka | 12.30±0.40(Predicted) | | color | White to light yellow |
| | BIX-02565 Usage And Synthesis |
| Uses | BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM. | | Biological Activity | bix 02565 is a novel inhibitor of ribosomal s6 kinase 2 with ic50 value of 1 nm [1].ribosomal s6 kinase (rsk) is a na/h exchanger (nhe) -activating factor and is important for ph maintenance during the early phase of cellular stress. while, nhe activation leads to ca2+ overload and cardiac hypertrophy over longer periods [2].bix 02565 is a novel rsk2 inhibitor. also, bix 02565 inhibited adrenergic ɑ1a-, ɑ1b-, ɑ1d-, ɑ2a-, β2- and imidazoline i2 receptors with ic50 values ranging from 0.052 to 1.820 μm. these receptors played important roles in the regulation of vascular tone and cardiac function [2]. also, bix 02565 inhibited lrrk2 and prkd1 with ic50 values of 16 and 35 nm [1].in the rat cv screen, bix 02565 (1, 3 and 10 mg/kg) significantly decreased heart rate (-93 +13 beats/min) and mean arterial pressure (map: to -65 +6 mm hg below baseline). in telemetry-instrumented rats, bix 02565 (30, 100 and 300 mg/kg for 4 days) reduced map (to -39 + 4 mm hg) in a concentration-dependent way [2]. | | in vivo | In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicits concentration-dependent decreases in MAP after each dose (to -39±4 mm Hg on day 4 at Tmax). BIX 02565 produces concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring at concentrations above 0.03 μM with a calculated EC50 of 3.1 μM. Subsequently, BIX 02565 is infused in the anesthetized rat in a low-dose (0.1, 0.3, and 1.0 mg/kg per 20 min) and high-dose (1.0, 3.0, and 10.0 mg/kg per 20 min) series of continuous infusions to test the effect of compound on hemodynamics in vivo[1]. | | IC 50 | RSK2 | | references | [1]. kirrane tm, boyer sj, burke j, et al. indole rsk inhibitors. part 2: optimization of cell potency and kinase selectivity. bioorg med chem lett, 2012, 22(1): 738-742.
[2]. fryer rm, muthukumarana a, chen rr, et al. mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal s6 kinase 2 inhibitors. j pharmacol exp ther, 2012, 340(3): 492-500. |
| | BIX-02565 Preparation Products And Raw materials |
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