2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. 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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TC-E 5005 Chemical Structure

TC-E 5005 Chemical Structure

CAS No. : 959705-64-7

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TC-E 5005 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

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[1].

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
Cell Line Type Value Description References
HEK293 IC50
17 nM
Compound: WEB-3
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
[PMID: 30587449]
Sf21 IC50
239 nM
Compound: Figure 16, R1C2
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
[PMID: 22834877]
Sf21 IC50
7 nM
Compound: Figure 16, R1C2
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
[PMID: 22834877]
Sf21 IC50
7.28 nM
Compound: 49
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
[PMID: 20450197]
Sf9 IC50
5540 nM
Compound: WEB-3
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
[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.

TC-E 5005 Related Antibodies
Molecular Weight

270.33

Formula

C15H18N4O
CAS No.
SMILES

COC1=CC=C2C(N3C(C(C)=N2)=C(C)N=C3CCC)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TC-E 5005 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-E 5005959705-64-7Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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