TC-E 5005
TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate.
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- No. CAS: 959705-64-7
- Fòrmula: C15H18N4O
- Peso molecular:270.33
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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PDE10A 7.28 nM (IC50) |
PDE2A 239 nM (IC50) |
hPDE11A 779 nM (IC50) |
PDE5A 919 nM (IC50) |
PDE7B 3100 nM (IC50) |
PDE3A 3700 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
17 nM
Compound: WEB-3
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Inhibition of recombinant human N-terminal His-tagged PDE10A2 expressed in HEK293 cells using cAMP as substrate measured after 60 mins
Inhibition of recombinant human N-terminal His-tagged PDE10A2 expressed in HEK293 cells using cAMP as substrate measured after 60 mins
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[PMID: 30587449] |
| Sf21 | IC50 |
239 nM
Compound: Figure 16, R1C2
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Inhibition of recombinant PDE2A expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
Inhibition of recombinant PDE2A expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
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[PMID: 22834877] |
| Sf21 | IC50 |
7 nM
Compound: Figure 16, R1C2
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Inhibition of recombinant PDE10A1 expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
Inhibition of recombinant PDE10A1 expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
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[PMID: 22834877] |
| Sf21 | IC50 |
7.28 nM
Compound: 49
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Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting
Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting
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[PMID: 20450197] |
| Sf9 | IC50 |
5540 nM
Compound: WEB-3
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Inhibition of human full-length PDE4D2 expressed in Sf9 insect cells using cAMP as substrate measured after 60 mins
Inhibition of human full-length PDE4D2 expressed in Sf9 insect cells using cAMP as substrate measured after 60 mins
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[PMID: 30587449] |
TC-E 5005 (500 nM) inhibits norepinephrine or phenylephrine and EFS (electric field stimulation)-induced contraction of human prostate strips[1].
TC-E 5005 (500 nM) shows amplification of treprostinil-induced relaxations, which were significant from 0.03 to 30 μM treprostinil[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 959705-64-7
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Peso molecular 270.33
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Fòrmula C15H18N4O
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SMILES
COC1=CC=C2C(N3C(C(C)=N2)=C(C)N=C3CCC)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-E 5005 Related Classifications
HY-10568 Related Classifications
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