RTI-7470-44
Based on 1 Customer Validation
RTI-7470-44 is an orally active and blood-brain barrier-permeable antagonist of trace amine-associated receptor 1 (hTAAR1) with a Ki of 0.3 nM. RTI-7470-44 inhibits hTAAR1-mediated cAMP production and signal transduction (IC50 = 8.4 nM), and blocks hTAAR1-mediated GIRK current responses. RTI-7470-44 increases the spontaneous firing frequency of dopaminergic neurons and reduces collagen-induced platelet aggregation. RTI-7470-44 can be used in studies related to Parkinson's disease and gastric emptying.
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: 99.85%
- CAS 番号: 825658-63-7
- 分子式: C19H11ClF3N5OS
- 分子量:449.84
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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GPCR/G Protein Compound Library
HY-L006
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CNS-Penetrant Compound Library
HY-L028
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Orally Active Compound Library
HY-L061
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Coagulation and Anti-coagulation Compound Library
HY-L136
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
生物活性
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TAAR1 8.4 nM (IC50) |
RTI-7470-44 potently and competitively inhibits hTAAR1-mediated cAMP production in hTAAR1-CHO cells, with an IC50 value of 8.4 nM[1].
RTI-7470-44 inhibits rTAAR1-mediated cAMP production in rTAAR1-HEK293 cells with an IC50 of 748 nM (as a potential non-competitive antagonist), and suppresses mTAAR1-mediated cAMP production in mTAAR1-HEK293 cells with an IC50 of 1190 nM[1].
RTI-7470-44 binds competitively to hTAAR1 membranes with a Ki value of 0.3 nM; it binds to mTAAR1 membranes with a Ki value of 139 nM, but enhances the binding of radioligands to rTAAR1 membranes[1].
RTI-7470-44 exhibits moderate affinity for rat BZP brain sites (Ki = 1 μM), extremely weak affinity for human sigma 2 receptors (Ki = 8.4 μM), and very low off-target activity against a panel of 42 other targets at a concentration of 10 μM[1].
RTI-7470-44 potently inhibits human TAAR1 with an EC50 of 167.6 nM[2].
RTI-7470-44 (40 nM) blocks TAAR1-mediated reduction of lipid accumulation, steatosis and phospholipidosis in differentiating 3T3-L1 adipocytes[2].
RTI-7470-44 (1 µM) weakly reverses Ralmitaront (HY-109157)-induced activation of GIRK channels in Xenopus oocytes expressing human TAAR1, reducing the response by 20%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 22-27 g)[2]
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Dosage:5 mg/kg (co-administered with JP-14 10 mg/kg); 5 mg/kg (single agent)
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Administration:i.g.; single dose
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Result:Reduced JP-14's inhibition of gastric emptying from ~66% to ~25%.
Did not affect gastric emptying when administered alone, with phenol red levels in the stomach comparable to vehicle controls.
化学情報
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CAS 番号 825658-63-7
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性状 Solid
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分子量 449.84
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分子式 C19H11ClF3N5OS
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Color Off-white to light yellow
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SMILES
N#CC1=C(SCC(NC2=NC=CC=N2)=O)N=C(C3=CC=C(Cl)C=C3)C=C1C(F)(F)F
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 20.83 mg/mL (46.31 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1].
Decker AM, et al. Identification of a Potent Human Trace Amine-Associated Receptor 1 Antagonist. ACS Chem Neurosci. 2022 Apr 6;13(7):1082-1095.
[Content Brief]
[2].
Marcinkowska M, et al. JP-14: A Trace Amine-Associated Receptor 1 Agonist with Anti-Metabolic Disorder Potential. Int J Mol Sci. 2025 Oct 15;26(20):10033.
[Content Brief]
[3].
Ågren R, et al. In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics. Int J Neuropsychopharmacol. 2023 Sep 25;26(9):599-606.
[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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2230 mL | 11.1151 mL | 22.2301 mL | 55.5753 mL |
| 5 mM | 0.4446 mL | 2.2230 mL | 4.4460 mL | 11.1151 mL | |
| 10 mM | 0.2223 mL | 1.1115 mL | 2.2230 mL | 5.5575 mL | |
| 15 mM | 0.1482 mL | 0.7410 mL | 1.4820 mL | 3.7050 mL | |
| 20 mM | 0.1112 mL | 0.5558 mL | 1.1115 mL | 2.7788 mL | |
| 25 mM | 0.0889 mL | 0.4446 mL | 0.8892 mL | 2.2230 mL | |
| 30 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8525 mL | |
| 40 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3894 mL |
RTI-7470-44 関連分類
HY-147319 関連分類
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