| 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%
BIX 02565 is a novel RSK2 inhibitor with IC50 of 1 nM. BIX 02565 inhibits adrenergic ɑ1A-, ɑ1B-, ɑ1D-, ɑ2A-, β2- and imidazoline I2 receptors with IC50 ranging from 0.052 to 1.820 μM. The regulation of cardiac and vascular tone depended heavily on these receptors.
| Targets |
RSK2 (IC50 = 1.1 nM)
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|---|---|
| ln Vitro |
BIX 02565 is a potent RSK2 inhibitor that, through indirect NHE inhibition, targets the treatment of heart failure secondary to myocardial infarction[1]. Its IC50 value is 1.1 nM. A second Rsk inhibitor, BIX 02565, guards against the reaction of biotinylated nucleotide acyl phosphates with enzyme active sites[2].
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| ln Vivo |
BIX 02565 causes concentration-dependent drops in MAP after each dose in telemetry-equipped rats (30, 100, and 300 mg/kg p.o. QD for 4 days), reaching -39±4 Hg at Tmax on day 4. At concentrations above 0.03 μM and an estimated EC50 of 3.1 μM, BIX 02565 causes concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring. The effect of the drug on hemodynamics is then tested in vivo by administering BIX 02565 to anesthetized rats 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[1].
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| Cell Assay |
MDS Pharma Services conducts radioligand binding studies. In selected assays (for BIX 02565) where inhibition of adrenergic binding generally exceeded 50%, an IC50 is determined by a nonlinear least-squares regression analysis. The mean percentage inhibition of specific binding or activity is shown for each assay tested. Briefly, Kinase GloPlus measures kinase activity using human RSK2 protein and quantifies residual ATP using a luciferin-luciferase-based detection reagent. The relative light unit signal is measured on an LJL Analyst in luminescence mode with a 384 aperture; relative light unit signals are converted to percentage of control; and the IC50 is fitted to a conventional four-parameter logistic equation[1].
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| Animal Protocol |
Rats: Male Sprague-Dawley rats (n=6) equipped with telemetry transmitters and conscious and mobile are used to measure mean arterial pressure. BIX 02565 is administered as a solution (10 mL/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle (30, 100, and 300 mg/kg p.o. QD). The compound is given at 0, 24, 48, and 72 hours; mean arterial pressure is recorded starting at 2 hours before (baseline) and continuing for 90 hours after the first dose. In order to perform a mass spectrometric analysis of the plasma drug concentrations on days 1 and 4, blood is drawn from satellite rats (n=3/group) at 1 hour after the dose (Tmax).
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| References |
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| Molecular Formula |
C26H30N6O2
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|---|---|
| Molecular Weight |
458.57
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| Exact Mass |
458.243
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| Elemental Analysis |
C, 68.10; H, 6.59; N, 18.33; O, 6.98
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| CAS # |
1311367-27-7
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| Related CAS # |
1311367-27-7
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| PubChem CID |
53246941
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| Appearance |
White to light yellow solid powder
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| LogP |
4.291
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
747
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C(C1=CC2=C(C=C1)C=C3N2[C@H](C)CCNC3=O)NC4=NC5=CC=CC=C5N4CCCN(C)C
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| InChi Key |
ZHMXXVNQAFCXKK-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C26H30N6O2/c1-17-11-12-27-25(34)23-15-18-9-10-19(16-22(18)32(17)23)24(33)29-26-28-20-7-4-5-8-21(20)31(26)14-6-13-30(2)3/h4-5,7-10,15-17H,6,11-14H2,1-3H3,(H,27,34)(H,28,29,33)/t17-/m1/s1
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| Chemical Name |
(5R)-N-[1-[3-(dimethylamino)propyl]benzimidazol-2-yl]-5-methyl-1-oxo-2,3,4,5-tetrahydro-[1,4]diazepino[1,2-a]indole-8-carboxamide
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| Synonyms |
BIX-02565; BIX02565;BIX 02565
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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 |
| 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: ~20.8 mg/mL (~45.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1807 mL | 10.9035 mL | 21.8069 mL | |
| 5 mM | 0.4361 mL | 2.1807 mL | 4.3614 mL | |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1807 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.
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