| Company Name: |
Changsha Fuzhen Biotechnology Co.，LTD Gold
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| Tel: |
15111215862 18229892877 |
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3062105966@qq.com |
| Products Intro: |
Product Name:RTI-7470-44
CAS:825658-63-7
Purity:98% Package:100mg，1g，5g 25g
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| | Acetamide, 2-[[6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)-2-pyridinyl]thio]-N-2-pyrimidinyl- Basic information |
| | Acetamide, 2-[[6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)-2-pyridinyl]thio]-N-2-pyrimidinyl- Chemical Properties |
| density | 1.54±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 20.83 mg/mL (46.31 mM; ultrasonic and warming and heat to 60°C) | | pka | 10.26±0.70(Predicted) | | form | Solid | | color | Off-white to light yellow | | InChI | InChI=1S/C19H11ClF3N5OS/c20-12-4-2-11(3-5-12)15-8-14(19(21,22)23)13(9-24)17(27-15)30-10-16(29)28-18-25-6-1-7-26-18/h1-8H,10H2,(H,25,26,28,29) | | InChIKey | WHNQNKYKDSLDKM-UHFFFAOYSA-N | | SMILES | C(NC1=NC=CC=N1)(=O)CSC1=NC(C2=CC=C(Cl)C=C2)=CC(C(F)(F)F)=C1C#N |
| | Acetamide, 2-[[6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)-2-pyridinyl]thio]-N-2-pyrimidinyl- Usage And Synthesis |
| Uses | RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD)[1]. | | Biological Activity | RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, drug addiction, and Parkinson's disease (PD)[1].
RTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (Ki=1 μM) and a very weak affinity for human sigma 2 (Ki=8.4 μM)[1].
RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist)[1].RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes[1].Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes[1]. species half-life (min) clearance, CLINT (mL/min/mg) Human83.914.9Rat9.11274Mouse65.863.5 | | in vivo | RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist)[1].
RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes[1].
Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes[1].
| species | half-life (min) | clearance, CLINT (mL/min/mg) | | Human | 83.9 | 14.9 | | Rat | 9.11 | 274 | | Mouse | 65.8 | 63.5 |
| | References | [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. |
| | Acetamide, 2-[[6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)-2-pyridinyl]thio]-N-2-pyrimidinyl- Preparation Products And Raw materials |
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