Art. -Nr.: HY-179390

KMCA-0011

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KMCA-0011 is an orally active ɑ_2C adrenoceptor antagonist (K_i = 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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Reinheit: 99.88%
Formel: C₂₂H₂₄ClN₃O₂
Molecular Weight:397.90

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

KMCA-0011 Chemical Structure

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Preis

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Alpha-2C adrenergic receptor

56.7 nM (Ki)

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

KMCA-0011 (Compound 11e) exhibits notably high binding affinity toward ɑ_2C Adrenoceptor (K_i = 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.

Western Blot Analysis^[1]

Cell Line:

ɑ_2C 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.

Chemical Information

Appearance Solid
Molecular Weight 397.90
Formel C₂₂H₂₄ClN₃O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5132 mL

12.5660 mL

25.1319 mL

5 mM

0.5026 mL

2.5132 mL

5.0264 mL

10 mM

0.2513 mL

1.2566 mL

2.5132 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Seo K, et al. ɑ2C Adrenoceptor antagonist KMCA-0011 alleviated depressive-like behaviors in a maternal separation mouse model. Bioorg Med Chem Lett. 2026 Feb 1;131:130467. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KMCA-0011

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KMCA-0011 Related Classifications

HY-179390 Related Classifications