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  4. RTI-7470-44

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).

For research use only. We do not sell to patients.

RTI-7470-44 Chemical Structure

RTI-7470-44 Chemical Structure

CAS No. : 825658-63-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
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RTI-7470-44 Related Antibodies

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Description

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].

IC50 & Target

IC50: 8.4 nM (human TAAR1), 748 nM (rat TAAR1), 1190 nM (mouse TAAR1)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RTI-7470-44 Related Antibodies
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

449.84

Formula

C19H11ClF3N5OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=C(SCC(NC2=NC=CC=N2)=O)N=C(C3=CC=C(Cl)C=C3)C=C1C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2230 mL 11.1151 mL 22.2301 mL
5 mM 0.4446 mL 2.2230 mL 4.4460 mL
View the 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.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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
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RTI-7470-44 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RTI-7470-44825658-63-7OthershTAAR1BBBventral tegmental areadopaminergic neuronsschizophreniadrug addictionParkinson’s diseaseRO5166017Inhibitorinhibitorinhibit

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