2. Membrane Transporter/Ion Channel
  3. HCN Channel
  4. MS7710

MS7710 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel inhibitor with blood-brain barrier permeability and an excellent brain/plasma concentration ratio. MS7710 inhibits HCN channel-mediated Ih current, and reduces the firing frequency and burst activity of dopaminergic neurons in the ventral tegmental area. MS7710 ameliorates chronic social defeat stress-induced deficits in social interaction and impairments in reward-related cognitive flexibility in mice. MS7710 exerts only limited effects on ventral tegmental area dopaminergic neuron activity, social interaction, exploratory behavior, locomotor activity or sucrose preference in control mice. MS7710 is applicable to the research of major depressive disorder.

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MS7710

MS7710 Chemical Structure

CAS No. : 3095336-10-7

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Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

MS7710 Related Antibodies

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Description

MS7710 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel inhibitor with blood-brain barrier permeability and an excellent brain/plasma concentration ratio. MS7710 inhibits HCN channel-mediated Ih current, and reduces the firing frequency and burst activity of dopaminergic neurons in the ventral tegmental area. MS7710 ameliorates chronic social defeat stress-induced deficits in social interaction and impairments in reward-related cognitive flexibility in mice. MS7710 exerts only limited effects on ventral tegmental area dopaminergic neuron activity, social interaction, exploratory behavior, locomotor activity or sucrose preference in control mice. MS7710 is applicable to the research of major depressive disorder[1][2].

In Vitro

MS7710 inhibits the firing frequency and burst activity of dopamine neurons in the ventral tegmental area (VTA) in brain slice electrophysiological experiments[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS7710 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Plasma Concentration
Mice[2] 20 mg/kg i.p. 0.82 0.79
Mice[2] 20 mg/kg i.p. 0.65 0.58
In Vivo

MS7710 (1-10 mg/kg; i.p.; single dose) significantly reduces hyperactive firing rate and bursting activity of ventral tegmental area dopamine neurons in male chronic social defeat stress-susceptible mice[2].
MS7710 (1 mg/kg; i.p.; single dose) significantly reduces hyperactive firing rate and bursting activity of ventral tegmental area dopamine neurons in female chronic social defeat stress-susceptible mice[2].
MS7710 (5 mg/kg; i.p.; single dose) produces long-lasting (14-day) amelioration of social interaction deficits and reward-related cognitive inflexibility in male and female chronic social defeat stress-susceptible mice[2].
MS7710 (20 mg/kg; i.p.; single dose) achieves a brain/plasma partition coefficient of 0.42 in male stress-naive mice and 0.21 in female stress-naive mice, demonstrating superior blood-brain barrier permeability relative to Cilobradine (HY-18940)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 8 weeks old, chronic social defeat stress-induced susceptible)[2]
Dosage: 1 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced ventral tegmental area dopamine neuron firing rate and bursting activity at 1 mg/kg compared to baseline.
Significantly reduced ventral tegmental area dopamine neuron firing rate and bursting activity at 10 mg/kg compared to baseline.
Animal Model: C57BL/6J (female, 8 weeks old, chronic social defeat stress-induced susceptible)[2]
Dosage: 1 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced ventral tegmental area dopamine neuron firing rate and bursting activity compared to baseline.
Animal Model: C57BL/6J (male and female, 8 weeks old, chronic social defeat stress-induced susceptible)[2]
Dosage: 5 mg/kg
Administration: i.p.; single dose
Result: Significantly increased social interaction ratios 14 days post-injection and improved probabilistic reversal reward learning task performance in male susceptible mice: required fewer sessions to re-establish preference for the new 80% reward lever and showed higher correct choice percentages during the reversal phase compared to saline controls.
Significantly increased social interaction ratios 14 days post-injection and improved probabilistic reversal reward learning task performance in female susceptible mice: required fewer sessions to re-establish preference for the new 80% reward lever and showed higher correct choice percentages during the reversal phase compared to saline controls.
Animal Model: C57BL/6J (male and female, 8 weeks old, stress-naive)[2]
Dosage: 20 mg/kg
Administration: i.p.; single dose
Result: Achieved a brain/plasma partition coefficient (Kp) of 0.42 in male mice and 0.21 in female mice, indicating significantly improved blood-brain barrier permeability compared to the parent compound Cilobradine.
Molecular Weight

468.59

Formula

C27H36N2O5
CAS No.
Appearance

Oil

Color

Off-white to light yellow

SMILES

COC1=CC=CC(OCCN2CCC[C@H](CN3C(CC(C=C(OC)C(OC)=C4)=C4CC3)=O)C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (213.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1341 mL 10.6703 mL 21.3406 mL
5 mM 0.4268 mL 2.1341 mL 4.2681 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (10.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (10.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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. 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
DMSO 1 mM 2.1341 mL 10.6703 mL 21.3406 mL 53.3515 mL
5 mM 0.4268 mL 2.1341 mL 4.2681 mL 10.6703 mL
10 mM 0.2134 mL 1.0670 mL 2.1341 mL 5.3352 mL
15 mM 0.1423 mL 0.7114 mL 1.4227 mL 3.5568 mL
20 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6676 mL
25 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1341 mL
30 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7784 mL
40 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
50 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
60 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 mL
80 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6669 mL
100 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5335 mL
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MS7710 Related Classifications

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  • 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:

MS77103095336-10-7MS 7710MS-7710HCN ChannelHyperpolarization activated cyclic nucleotide gated channelsreward-associated cognitive inflexibilitysocial interaction deficitshyperpolarization-activatedcyclic nucleotide-gated (HCN) channelchronic social defeat stressmale miceventral tegmental area dopamine neuronsmajor depressive disorderfemale miceblood-brain barrierInhibitorinhibitorinhibit

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