Cilobradine hydrochloride
Based on 1 Customer Validation
Cilobradine hydrochloride is a HCN channel blocker. Cilobradine hydrochloride induces cardiac pacemaker currents and produces antidepressant effects.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 186097-54-1
- Formula: C28H39ClN2O5
- Molecular Weight:519.07
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Cilobradine (1 μM) hydrochloride induces a use-dependent blockade of cardiac pacemaker current in rabbit sino-atrial cells[2].
Cilobradine blocks HCN channel currents in HEK293 cells expressing human HCN1, HCN2, HCN3, and HCN4 channels in a dose- and treatment-dependent manner, and its steady-state inhibition of different HCN isoforms is not isoform-specific[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
. Cilobradine (intracerebroventricular injection dose 0.6 μg; intraperitoneal injection dose 20 mg/kg; intracerebroventricular microinjection and i.p.; single dose) hydrochloride can reverse depressive-like behavior, and the effect lasts for about two weeks[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (8-15 weeks old), chronic social defeat stress (CSDS) model[5]
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Dosage:Intra-VTA injection 0.6 μg, intraperitoneal injection 20 mg/kg
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Administration:Intra-VTA micro- infusion or intraperitoneal injection, single
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Result:Reversed depressive-like behaviors within 1 h and the effect lasted for about two weeks.
Increased time in social interaction and reduced time in the corner zone.
Increased sucrose preference and reduced immobility time in the forced swim test.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 186097-54-1
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Appearance Solid
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Molecular Weight 519.07
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Formula C28H39ClN2O5
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Color White to off-white
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SMILES
O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl
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Synonyms
DK-AH 269
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL (240.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (192.65 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Cheng L, et al. Molecular mapping of the binding site for a blocker of hyperpolarization-activated, cyclic nucleotide-modulated pacemaker channels. J Pharmacol Exp Ther. 2007 Sep;322(3):931-939. [Content Brief]
[2]. Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003 Oct 8;478(2-3):161-71. [Content Brief]
[3]. Stieber J, et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006 Apr;69(4):1328-37. [Content Brief]
[4]. Umeya N, et al. Detection of retinal dysfunction induced by HCN channel inhibitors using multistep light stimulus and long-duration light stimulus ERG in rats. Exp Eye Res. 2024 Apr;241:109847. [Content Brief]
[5]. Cai M, et al. HCN channel inhibitor induces ketamine-like rapid and sustained antidepressant effects in chronic social defeat stress model. Neurobiol Stress. 2023 Aug 19;26:100565. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9265 mL | 9.6326 mL | 19.2652 mL | 48.1631 mL |
| 5 mM | 0.3853 mL | 1.9265 mL | 3.8530 mL | 9.6326 mL | |
| 10 mM | 0.1927 mL | 0.9633 mL | 1.9265 mL | 4.8163 mL | |
| 15 mM | 0.1284 mL | 0.6422 mL | 1.2843 mL | 3.2109 mL | |
| 20 mM | 0.0963 mL | 0.4816 mL | 0.9633 mL | 2.4082 mL | |
| 25 mM | 0.0771 mL | 0.3853 mL | 0.7706 mL | 1.9265 mL | |
| 30 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6054 mL | |
| 40 mM | 0.0482 mL | 0.2408 mL | 0.4816 mL | 1.2041 mL | |
| 50 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9633 mL | |
| 60 mM | 0.0321 mL | 0.1605 mL | 0.3211 mL | 0.8027 mL | |
| 80 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6020 mL | |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1927 mL | 0.4816 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Cilobradine hydrochloride Related Classifications
HY-18940A Related Classifications
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