| 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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Zatebradine HCl (UL-FS 49; UL-FS 49CL), the hydrochloride salt of Zatebradine, is a novel and potent bradycardic agent which inhibits hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. . It blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells.
| ln Vitro |
In rabbit sinoatrial node cells, zatebradine exhibits an apparent Kd of 480 nM for usage-dependent inhibition of cardiac pacemaker currents [2].
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|---|---|
| ln Vivo |
Zatebradine (0–20 mg/kg; intraperitoneally; 30 min; male C57/Bl6 mice) increased cardiac arrhythmias and dose-dependently decreased heart rate from 600 to 200 bpm (ED50 = 1.8 mg/kg) [1].
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| Animal Protocol |
Animal/Disease Models: Male C57/Bl6-mouse[1]
Doses: 0mg/kg, 0.1mg/kg, 1mg/kg, 10mg/kg, 20mg/kg Route of Administration: intraperitoneal (ip) injection; 30 minutes Experimental Results: Acute blood glucose was observed diminished, dose-dependent reductions in glycated hemoglobin Dramatically prevented the reduction in IRI levels at the 3 and 10 mg/kg doses, with no differences in food intake or body weight. |
| References |
| Molecular Formula |
C26H37CLN2O5
|
|---|---|
| Molecular Weight |
493.03538
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| Exact Mass |
492.239
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| CAS # |
91940-87-3
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| Related CAS # |
Zatebradine;85175-67-3
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| PubChem CID |
3045335
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.115g/cm3
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| Boiling Point |
612.5ºC at 760mmHg
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| Flash Point |
324.3ºC
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| LogP |
3.952
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
34
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZRNKXJHEQKMWCH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H36N2O5.ClH/c1-27(13-9-19-7-8-22(30-2)23(15-19)31-3)11-6-12-28-14-10-20-16-24(32-4)25(33-5)17-21(20)18-26(28)29/h7-8,15-17H,6,9-14,18H2,1-5H31H
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| Chemical Name |
3-[3-[2-(3,4-Dimethoxyphenyl)ethyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one hydrochloride
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| Synonyms |
Zatebradine HCl UL-FS49 UL FS49Zatebradine Hydrochloride ULFS49
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~202.82 mM)
DMSO : ~100 mg/mL (~202.82 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.07 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 25.0 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: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (223.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0282 mL | 10.1412 mL | 20.2823 mL | |
| 5 mM | 0.4056 mL | 2.0282 mL | 4.0565 mL | |
| 10 mM | 0.2028 mL | 1.0141 mL | 2.0282 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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