THPP-1
Based on 1 publication(s) in Google Scholar
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.75%
- CAS 番号: 1257051-63-0
- 分子式: C23H21ClN6O3
- 分子量:464.90
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 THPP-1
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生物活性
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PDE10 |
THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases phosphorylation of GluR1 S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g[1].
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Dosage:0.1-1.0 mg/kg.
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Administration:P.O.
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Result:Showed novel object recognition.
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Animal Model:Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit
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Dosage:1, 3, 10 mg/kg.
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Administration:P.O.
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Result:Significantly attenuated the stimulant effects in SIMA.
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Animal Model:Male Wistar Hannover rats ranging from 200 to 300 g[1].
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Dosage:1-30 mg/kg.
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Administration:P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (Pharmacokinetic Analysis).
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Result:Dose-dependently increases phosphorylation of GluR1 S845.
化学情報
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CAS 番号 1257051-63-0
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性状 Solid
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分子量 464.90
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分子式 C23H21ClN6O3
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Color Off-white to light yellow
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SMILES
O=C(C1=C2C=CC=CN2C=N1)N3CCC4=NC(C5=CC=C(N=C5)Cl)=NC(OCCOC)=C4C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175
溶剤 & 溶解度
DMSO : 31.25 mg/mL (67.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Smith SM, et al. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey. Neuropharmacology. 2013 Jan;64:215-23. [Content Brief]
[2]. Vardigan JD, et al. Behavioral and qEEG effects of the PDE10A inhibitor THPP-1 in a novel rhesus model of antipsychotic activity. Psychopharmacology (Berl). 2016 Jul;233(13):2441-50. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1510 mL | 10.7550 mL | 21.5100 mL | 53.7750 mL |
| 5 mM | 0.4302 mL | 2.1510 mL | 4.3020 mL | 10.7550 mL | |
| 10 mM | 0.2151 mL | 1.0755 mL | 2.1510 mL | 5.3775 mL | |
| 15 mM | 0.1434 mL | 0.7170 mL | 1.4340 mL | 3.5850 mL | |
| 20 mM | 0.1076 mL | 0.5378 mL | 1.0755 mL | 2.6888 mL | |
| 25 mM | 0.0860 mL | 0.4302 mL | 0.8604 mL | 2.1510 mL | |
| 30 mM | 0.0717 mL | 0.3585 mL | 0.7170 mL | 1.7925 mL | |
| 40 mM | 0.0538 mL | 0.2689 mL | 0.5378 mL | 1.3444 mL | |
| 50 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0755 mL | |
| 60 mM | 0.0359 mL | 0.1793 mL | 0.3585 mL | 0.8963 mL |
THPP-1 関連分類
HY-117604 関連分類
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