2. GPCR/G Protein Neuronal Signaling Others
  3. Orexin Receptor (OX Receptor) Isotope-Labeled Compounds
  4. Tebideutorexant

Tebideutorexant  (Synonyms: JNJ-61393215)

Cat. No.: HY-147403S Purity: 98.95%
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Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders.

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

Tebideutorexant

Tebideutorexant Chemical Structure

CAS No. : 1637681-55-0

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Tebideutorexant Related Antibodies

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Description

Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

In Vitro

Tebideutorexant (JNJ-61393215) exhibits high affinity, potency, and selectivity for human and rat OX1R over OX2R and other molecular targets in vitro[1].

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

Tebideutorexant Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration
Rat[1] 0.1, 1, 10 mg/kg p.o. 34 ng/mL
Rat[1] 10, 30 mg/kg p.o. 535 ng/mL
In Vivo

Tebideutorexant (3-30 mg/kg; p.o., single dose) dose-dependently blocks CO2-induced fear and bradycardia in rats, with efficacy at 10 and 30 mg/kg[1].
Tebideutorexant (0.1-10 mg/kg; p.o.) shows dose- and time-dependent brain OX1R occupancy in rats, with oral bioavailability and brain penetration[1].
Tebideutorexant (10 mg/kg; p.o.) reduces NREM and REM sleep latency without altering total sleep duration in rats[1].
Tebideutorexant (30 mg/kg; p.o.) selectively promotes REM sleep in OX2R KO mice, demonstrating in vivo OX1R target engagement[1].

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

Animal Model: Sprague-Dawley (male, 300-400 g)[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o., single dose
Result: Blocked CO₂-induced reduction in social interaction behaviors at 10 and 30 mg/kg; attenuated CO₂-induced bradycardia responses at 8 and 9 minutes post-challenge at 30 mg/kg.
Animal Model: Sprague-Dawley (male, 300-400 g)[1]
Dosage: 0.1, 1, 10 mg/kg
Administration: p.o., single dose
Result: Produced time- and dose-dependent brain OX1R occupancy; reached 89% maximal occupancy at 15 minutes and remained above 47% for 8 hours at 10 mg/kg; achieved plasma EC50 of 34 ng/mL for 50% occupancy.
Animal Model: Sprague-Dawley (male, 350-450 g)[1]
Dosage: 10 mg/kg
Administration: p.o., single dose
Result: Did not alter total NREM or REM sleep duration; significantly decreased NREM and REM sleep latency.
Animal Model: C57Bl6 OX2R knockout (male, 30-35 g, OX2R KO model)[1]
Dosage: 30 mg/kg
Administration: p.o., single dose
Result: Significantly reduced REM sleep latency; prolonged REM sleep duration in the first 2 hours post-treatment; showed no effect on NREM sleep parameters.
Molecular Weight

460.42

Formula

C23H16D2F4N4O2
CAS No.
Unlabeled CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C2=NC=CC=N2)C(F)=CC=C1)N3[C@@H]4[C@@H](C[C@H](C3([2H])[2H])C4)OC5=CC=C(C=N5)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Tebideutorexant Related Classifications

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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:

Tebideutorexant1637681-55-0JNJ-61393215JNJ61393215JNJ 61393215Orexin Receptor (OX Receptor)Isotope-Labeled CompoundsHypocretin ReceptorHCRT Receptorhuman OX1Rrat OX1Rpanic disordersOX2ROX1ROX2R KO miceanxiety disordersanxiety symptomspanic-like behaviorratsInhibitorinhibitorinhibit

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