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.
For research use only. We do not sell to patients.
- CAS No.: 959705-64-7
- Formula: C15H18N4O
- Molecular Weight:270.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
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) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
Chemical Information
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CAS No. 959705-64-7
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Molecular Weight 270.33
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Formula C15H18N4O
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SMILES
COC1=CC=C2C(N3C(C(C)=N2)=C(C)N=C3CCC)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-E 5005 Related Classifications
HY-10568 Related Classifications
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