TC-E 5005

Potent and selective PDE10A inhibitor CAS# 959705-64-7

TC-E 5005

Catalog No. BCC6227----Order now to get a substantial discount!

Product Name & Size Price Stock
TC-E 5005: 5mg $115 In Stock
TC-E 5005: 10mg Please Inquire In Stock
TC-E 5005: 20mg Please Inquire Please Inquire
TC-E 5005: 50mg Please Inquire Please Inquire
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Chemical structure

TC-E 5005

3D structure

Chemical Properties of TC-E 5005

Cas No. 959705-64-7 SDF Download SDF
PubChem ID 24802717 Appearance Powder
Formula C15H18N4O M.Wt 270.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in 1eq. HCl and to 100 mM in ethanol
SMILES CCCC1=NC(=C2N1C3=C(C=CC(=N3)OC)N=C2C)C
Standard InChIKey YNADXFWEXJTQSZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H18N4O/c1-5-6-12-17-10(3)14-9(2)16-11-7-8-13(20-4)18-15(11)19(12)14/h7-8H,5-6H2,1-4H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TC-E 5005

DescriptionPotent and selective PDE10A inhibitor (IC50 values are 7.28, 239, 779, 919, 3100 and 3700 nM at PDE10A, 2A, 11A, 5A, 7B and 3A respectively and >5000 nM at PDE1B, 4A, 6, 8A and 9A). Reverses MK 801-induced hyperactivity in vivo.

TC-E 5005 Dilution Calculator

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TC-E 5005 Molarity Calculator

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Preparing Stock Solutions of TC-E 5005

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.6992 mL 18.4959 mL 36.9918 mL 73.9836 mL 92.4796 mL
5 mM 0.7398 mL 3.6992 mL 7.3984 mL 14.7967 mL 18.4959 mL
10 mM 0.3699 mL 1.8496 mL 3.6992 mL 7.3984 mL 9.248 mL
50 mM 0.074 mL 0.3699 mL 0.7398 mL 1.4797 mL 1.8496 mL
100 mM 0.037 mL 0.185 mL 0.3699 mL 0.7398 mL 0.9248 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on TC-E 5005

Inhibition of Adrenergic and Non-Adrenergic Smooth Muscle Contraction in the Human Prostate by the Phosphodiesterase 10-Selective Inhibitor TC-E 5005.[Pubmed:27418235]

Prostate. 2016 Nov;76(15):1364-74.

BACKGROUND: The phosphodiesterase (PDE) 5 inhibitor tadalafil is available for treatment of male lower urinary tract symptoms (LUTS), while the role of other PDE isoforms for prostate smooth muscle tone is still unknown. Here, we examined effects of the PDE10-selective inhibitor TC-E 5005 on smooth muscle contraction in human prostate tissue. METHODS: Prostate samples were obtained from patients undergoing radical prostatectomy. Expression of PDE10 was addressed by RT-PCR, Western blot, and fluorescence staining with different markers. Effects of TC-E 5005 and tadalafil on contraction, and relaxation of prostate strips were studied via organ bath. RESULTS: PDE10A was detectable by RT-PCR, Western blot, and fluorescence staining in prostate tissues. Colocalization with markers suggested expression of PDE10A in smooth muscle cells and catecholaminergic nerves. Norepinephrine, the alpha1 -adrenergic agonist phenylephrine, the thromboxane A2 analogue U46619, and endothelins 1-3 induced concentration-dependent contractions of prostate strips, while electric field stimulation (EFS) induced frequence-dependent contractions. Application of TC-E 5005 (500 nM) caused significant inhibition of norepinephrine-, phenylephrine-, and endothelin-3-induced contractions. Inhibition of EFS-induced contractions by TC-E 5005 ranged around 50%, resembling inhibition of EFS-induced contractions by tadalafil (10 muM). The prostacyclin analog treprostinil and the nitric oxide donor DEA NONOate induced relaxations of precontracted prostate strips, which were significantly amplified by TCE 5005. CONCLUSIONS: The PDE10-selective inhibitor TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate. TC-E 5005 inhibits neurogenic contractions with similar efficacy than tadalafil, so that urodynamic effects in vivo appear possible. Prostate 76:1364-1374, 2016. (c) 2016 Wiley Periodicals, Inc.

Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.[Pubmed:20450197]

J Med Chem. 2010 Jun 10;53(11):4399-411.

Novel imidazo[1,5-a]pyrido[3,2-e]pyrazines have been synthesized and characterized as both potent and selective phosphodiesterase 10A (PDE10A) inhibitors. For in vitro characterization, inhibition of PDE10A mediated cAMP hydrolysis was used and a QSAR model was established to analyze substitution effects. The outcome of this analysis was complemented by the crystal structure of PDE10A in complex with compound 49. Qualitatively new interactions between inhibitor and binding site were found, contrasting with previously published crystal structures of papaverine-like inhibitors. In accordance with the known antipsychotic potential of PDE10A inhibitors, MK-801 induced stereotypy and hyperactivity in rats were reversed by selected compounds. Thus, a promising compound class has been identified for the treatment of schizophrenia that could circumvent side effects connected with current therapies.

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