KMCA-0011
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.88%
- Formule: C22H24ClN3O2
- Masse moléculaire:397.90
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Alpha-2C adrenergic receptor 56.7 nM (Ki) |
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.
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Cell Line:ɑ2C Adrenoceptor cDNA-transfected HEK-293 cells
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Concentration:10 μM
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Incubation Time:
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Result:Induced no detectable ERK phosphorylation, indicating the absence of agonist activity.
Inhibited Epinephrine-induced ERK phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Maternal separation (MS) mouse model in ICR mice (7 weeks)[1]
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Dosage:1, 3, 10 mg/kg
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Administration:oral gavage (p.o.), daily for one week
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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
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Appearance Solid
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Masse moléculaire 397.90
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Formule C22H24ClN3O2
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Color White to off-white
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SMILES
ClC1=CC=C(OC(C(NCCN2CCC(CC3=CC=CC=C3)CC2)=O)=N4)C4=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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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