2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)
  4. RTI-7470-44

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.

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RTI-7470-44

RTI-7470-44 Chemical Structure

CAS No. : 825658-63-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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RTI-7470-44 Related Antibodies

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Description

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[1].

IC50 & Target[1]

TAAR1

8.4 nM (IC50)

In Vitro

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.

RTI-7470-44 Related Antibodies
In Vivo

RTI-7470-44 (5 mg/kg; i.g.; single dose) partially attenuates the gastric emptying-inhibiting effect of the TAAR1 agonist JP-14 in mice, reducing the inhibition rate to 25%[2].

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

Animal Model: C57BL/6 (male, 22-27 g)[2]
Dosage: 5 mg/kg (co-administered with JP-14 10 mg/kg); 5 mg/kg (single agent)
Administration: i.g.; single dose
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.
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-7470-44825658-63-7Trace Amine-associated Receptor (TAAR)human Trace Amine-Associated Receptor 1hTAAR1-CHO cellsParkinson’s diseasemTAAR1-HEK293 cellsrTAAR1-HEK293 cellsHepG2 cells3T3-L1 adipocytesMDCK-mdr1 cell monolayershTAAR1dopaminergic neuronsInhibitorinhibitorinhibit

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