JD03-02
JD03-02 is an orally active, blood-brain barrier-permeable TRPC1/5 heterodimer inhibitor with an IC50 of 0.2 nM. JD03-02 preferentially binds to a unique ligand-binding pocket at the interface of TRPC1-TRPC5, exerts almost no inhibitory effect on TRPC5 homotetramers, and thus avoids side effects such as obesity and hyperkinesia. JD03-02 induces anxiolytic and antidepressant effects in mouse models. JD03-02 can be used in studies related to depression and anxiety disorders.
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- Formule: C25H27Cl2N5O3
- Masse moléculaire:516.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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TRPC1/5 0.2 nM (IC50) |
TRPC1/4 6.7 nM (IC50) |
TRPC5 8504 nM (IC50) |
TRPC4 2385 nM (IC50) |
JD03-02 (10 μM) potently inhibits TRPC1/5 heteromer-mediated calcium influx in HEK293T cells, whereas it exerts no effect on TRPC5 homomers at the concentration of 10 μM[1].
JD03-02 potently inhibits TRPC1/5 heteromers in HEK293T cells with an IC50 of 0.2 nM, and exhibits over 10000-fold selectivity over TRPC5 homomers (IC50 = 8504 nM)[1].
JD03-02 inhibits TRPC1/4 heteromers in HEK293T cells with an IC50 of 6.7 nM, and exhibits selectivity for TRPC4 homomers (IC50 = 2385 nM)[1].
JD03-02 (10 μM) exhibits only extremely low activity against human TRPC3, TRPC6 and TRPC7, with an inhibition rate of no more than 40% at a concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JD03-02 (3-30 mg/kg; p.o.; single administration) exerts dose-dependent anxiolytic effects in mCPP (HY-101324)-induced anxiety-like mice[1].
JD03-02 (10 mg/kg; p.o.; once daily; 11 days) does not induce weight gain or hyperphagia in diet-induced obese mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 7-8 weeks old, chronic unpredictable mild stress-induced depression model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg (single dose; daily for 14 days)
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Administration:p.o.; daily (14 days); single dose
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Result:Significantly increased sucrose preference compared to vehicle control after a single 30 mg/kg dose.
Significantly increased sucrose preference compared to vehicle control after 11 days of daily treatment with 3 mg/kg, 10 mg/kg, and 30 mg/kg doses, with the 30 mg/kg dose showing greater improvement than the 3 mg/kg dose.
Significantly reduced immobility time in the forced swim test compared to vehicle control after 14 days of daily treatment with 3 mg/kg, 10 mg/kg, and 30 mg/kg doses, with the 30 mg/kg dose showing greater improvement than the 3 mg/kg dose.
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Animal Model:C57BL/6J (male, 7-8 weeks old, mCPP-induced anxiety model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently increased open arm entries and time spent in open arms in the elevated plus maze compared to vehicle control.
Dose-dependently reduced the number of marbles buried in the marble burying test compared to vehicle control.
Dose-dependently increased central zone entries and time spent in the central zone in the open field test compared to vehicle control.
Showed significantly superior efficacy to diazepam in the open field test at 30 mg/kg.
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Animal Model:C57BL/6J (male, 14 weeks old, high-fat diet-induced obesity model)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 11 days
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Result:Had no significant effect on body weight compared to vehicle control.
Had no significant effect on daily or cumulative food intake compared to vehicle control.
Chemical Information
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Masse moléculaire 516.42
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Formule C25H27Cl2N5O3
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SMILES
CN(CCCCN1C(C2=C(N(C1=O)C)N=C(N2CC3=CC=C(C=C3)Cl)OC4=CC=CC(Cl)=C4)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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