2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. KMCA-0011

KMCA-0011 is an orally active ɑ2C adrenoceptor antagonist (Ki = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression.

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KMCA-0011

KMCA-0011 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

KMCA-0011 Related Antibodies

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Description

KMCA-0011 is an orally active ɑ2C adrenoceptor antagonist (Ki = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression[1].

IC50 & Target[1]

Alpha-2C adrenergic receptor

56.7 nM (Ki)

In Vitro

KMCA-0011 (Compound 11e) exhibits notably high binding affinity toward ɑ2C Adrenoceptor (Ki = 56.7 nM) in human HEK-293 cells[1].
KMCA-0011 (10 μM) effectively inhibits Epinephrine-induced (HY-B0447) ERK phosphorylation[1].

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

KMCA-0011 Related Antibodies

Western Blot Analysis[1]

Cell Line: ɑ2C Adrenoceptor cDNA-transfected HEK-293 cells
Concentration: 10 μM
Incubation Time:
Result: Induced no detectable ERK phosphorylation, indicating the absence of agonist activity.
Inhibited Epinephrine-induced ERK phosphorylation.
In Vivo

KMCA-0011 (Compound 11e) (1-10 mg/kg, p.o., daily for one week) shows the most consistent behavioral efficacy across multiple tests, uniquely ameliorates anxiety-like behavior in the EPM test, increases hippocampal BDNF expression and restores CORT-induced impairments in synaptic plasticity in the Maternal separation (MS) mouse model[1].

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

Animal Model: Maternal separation (MS) mouse model in ICR mice (7 weeks)[1]
Dosage: 1, 3, 10 mg/kg
Administration: oral gavage (p.o.), daily for one week
Result: Exhibited rapid antidepressant-like effects after a single administration, accompanied by enhanced synaptic plasticity.
Markedly improved cognitive dysfunction and reduced immobility time at all tested doses.
Neither decreased distance moved nor induced hyperactivity-like side effects.
Showed the most pronounced effect at 3 mg/kg, suggesting an improvement in anhedonia.
Restored sociability at 10 mg/kg.
Specifically improved MS-induced anxiety.
Significantly elevated BDNF expression at 10 mg/kg, indicating antidepressant activity through BDNF signaling modulation.
Effectively reversed the CORT-induced LTP impairment.
Molecular Weight

397.90

Formula

C22H24ClN3O2
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(OC(C(NCCN2CCC(CC3=CC=CC=C3)CC2)=O)=N4)C4=C1
Shipping

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

DMSO : 50 mg/mL (125.66 mM; ultrasonic and warming and heat to 60°C; 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 2.5132 mL 12.5660 mL 25.1319 mL
5 mM 0.5026 mL 2.5132 mL 5.0264 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (12.57 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    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% Corn Oil

    Solubility: ≥ 5 mg/mL (12.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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 2.5132 mL 12.5660 mL 25.1319 mL 62.8299 mL
5 mM 0.5026 mL 2.5132 mL 5.0264 mL 12.5660 mL
10 mM 0.2513 mL 1.2566 mL 2.5132 mL 6.2830 mL
15 mM 0.1675 mL 0.8377 mL 1.6755 mL 4.1887 mL
20 mM 0.1257 mL 0.6283 mL 1.2566 mL 3.1415 mL
25 mM 0.1005 mL 0.5026 mL 1.0053 mL 2.5132 mL
30 mM 0.0838 mL 0.4189 mL 0.8377 mL 2.0943 mL
40 mM 0.0628 mL 0.3141 mL 0.6283 mL 1.5707 mL
50 mM 0.0503 mL 0.2513 mL 0.5026 mL 1.2566 mL
60 mM 0.0419 mL 0.2094 mL 0.4189 mL 1.0472 mL
80 mM 0.0314 mL 0.1571 mL 0.3141 mL 0.7854 mL
100 mM 0.0251 mL 0.1257 mL 0.2513 mL 0.6283 mL
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KMCA-0011 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:

KMCA-0011KMCA0011KMCA 0011Adrenergic ReceptorBeta Receptorɑ2CadrenoceptorAntagonistAntidepressantMolecular dockingMaternal separation mouseInhibitorinhibitorinhibit

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