2. Membrane Transporter/Ion Channel
  3. HCN Channel
  4. Cilobradine hydrochloride

Cilobradine hydrochloride  (Synonyms: DK-AH 269)

Cat. No.: HY-18940A Purity: 99.73%
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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.

Cilobradine hydrochloride Chemical Structure

Cilobradine hydrochloride Chemical Structure

CAS No. : 186097-54-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Cilobradine hydrochloride:

Cilobradine hydrochloride Related Antibodies

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Description

Cilobradine hydrochloride is a HCN channel blocker. Cilobradine hydrochloride induces cardiac pacemaker currents and produces antidepressant effects[1][2][3][4][5].

In Vitro

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 hydrochloride Related Antibodies
In Vivo

Cilobradine (4-40 mg/kg; s.c,; single dose) hydrochloride can prolong the latency of the a-wave or b-wave of the rat electroretinogram (ERG), and a dose-dependent waveform change after the b-wave occurs at a specific light stimulus brightness[4].
. 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.

Animal Model: Male C57BL/6J mice (8-15 weeks old), chronic social defeat stress (CSDS) model[5]
Dosage: Intra-VTA injection 0.6 μg, intraperitoneal injection 20 mg/kg
Administration: Intra-VTA micro- infusion or intraperitoneal injection, single
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.
Clinical Trial
Molecular Weight

519.07

Formula

C28H39ClN2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9265 mL 9.6326 mL 19.2652 mL
5 mM 0.3853 mL 1.9265 mL 3.8530 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.73%

SDS (252 KB)

COA (247 KB) HNMR (251 KB) LCMS (100 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)
References

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.

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Cilobradine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cilobradine186097-54-1DK-AH 269HCN ChannelHyperpolarization activated cyclic nucleotide gated channelsInhibitorinhibitorinhibit

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