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KMCA-0011 is an orally active antagonist of the ɑ2C adrenoceptor (Ki= 56.7 nM). It alleviates depressive behavior by enhancing brain-derived neurotrophic factor (BDNF) and synaptic plasticity. KMCA-0011 demonstrates excellent metabolic stability, maintaining 99.8% plasma stability after 120 minutes. It is a useful compound for researching depression.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | KMCA-0011 is an orally active antagonist of the ɑ2C adrenoceptor (Ki= 56.7 nM). It alleviates depressive behavior by enhancing brain-derived neurotrophic factor (BDNF) and synaptic plasticity. KMCA-0011 demonstrates excellent metabolic stability, maintaining 99.8% plasma stability after 120 minutes. It is a useful compound for researching depression. |
| Targets&IC50 | α2C-adrenoceptor:56.7 nM (Ki) |
| In vitro | KMCA-0011 (Compound 11e) demonstrates significant high binding affinity for ɑ2C adrenoceptors in human HEK-293 cells (K i = 56.7 nM). At a concentration of 10 μM, KMCA-0011 effectively inhibits adrenaline-induced ERK phosphorylation. |
| In vivo | KMCA-0011 (Compound 11e), administered orally at a dosage of 1-10 mg/kg once daily for one week, consistently demonstrated therapeutic efficacy across several tests. It uniquely reduced anxiety-like behavior in the EPM test, enhanced hippocampal BDNF expression, and restored CORT-induced synaptic plasticity impairments in the mother-offspring separation (MS) mouse model. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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