1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. TC-E 5005

TC-E 5005 是一种有效的选择性 PDE10A 抑制剂,对 PDE10A、2A、11A、5A、7B 和 3A 的 IC50 值分别为 7.28、239、779、919、3,100 和 3,700 nM。TC-E 5005 抑制人前列腺中的肾上腺素能和神经源性平滑肌收缩。

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TC-E 5005 Chemical Structure

TC-E 5005 Chemical Structure

CAS No. : 959705-64-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

270.33

Formula

C15H18N4O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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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.

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TC-E 5005
目录号:
HY-10568
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