2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline
- Product Name
- 2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline
- CAS No.
- 898563-00-3
- Chemical Name
- 2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline
- Synonyms
- TP-10;TP-10, 10 mM in DMSO;2-[[4-[4-pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline;2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline;2-({4-[4-(4-Pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]p henoxy}methyl)quinoline;Quinoline, 2-[[4-[4-(4-pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]phenoxy]methyl]-;schizophrenia,U-87 MG,TP 10,cGMP,TP10,inhibit,TP-10,disorder,Inhibitor,cAMP,reactive oxygen,Phosphodiesterase (PDE),pCREB-LI
- CBNumber
- CB82535186
- Molecular Formula
- C26H19F3N4O
- Formula Weight
- 460.45
- MOL File
- 898563-00-3.mol
2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline Property
- Boiling point:
- 564.4±50.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 100 mg/mL (217.18 mM);Water : < 0.1 mg/mL (insoluble)
- pka
- 4.08±0.10(Predicted)
- form
- Solid
- color
- Light yellow to brown
N-Bromosuccinimide Price
- Product number
- CS-5242
- Product name
- TP-10
- Purity
- 98.54%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- HCH0316639
- Product name
- TP-10
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $499.36
- Updated
- 2021/12/16
- Product number
- CS-5242
- Product name
- TP-10
- Purity
- 98.54%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-5242
- Product name
- TP-10
- Purity
- 98.54%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- CS-5242
- Product name
- TP-10
- Purity
- 98.54%
- Packaging
- 100mg
- Price
- $2520
- Updated
- 2021/12/16
2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline Chemical Properties,Usage,Production
Description
TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM.IC50 value: 0.8 nM [1]Target: PDE10ATP-10 has extremely potent PDE10A inhibitory activity and highselectivity against other PDEs, and be active in the mouse behavioral model for positive symptoms. TP-10 demonstrats good in vitro and in vivo activity, the intrinsic clearance (CLint) of these compounds in mouse liver microsomes (MLM) was extremely high in assay (CLint>1000 mL/min/kg). [1]
Uses
TP-10 is a selective PDE10A inhibitor with an IC50 value of 0.8 nM. TP-10 shows an antioxidant activity with IC50s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy[1][2][3].
in vivo
TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides[2].
| Animal Model: | Male CD rats[2] |
| Dosage: | 0.1, 0.32, 1.0, 3.2 and 10 mg/kg |
| Administration: | Subcutaneous injection; 0.1-10 mg/kg once |
| Result: | Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg. |
References
[1]. Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213. [2]. Verhoest PR, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem
2-{4-[4-Pyridin-4-yl-1-(2,2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline Preparation Products And Raw materials
Raw materials
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