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

Tebideutorexant  (Synonyms: JNJ-61393215)

製品番号: HY-147403S 純度: 98.95%
COA 取扱説明書 Technical Support

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.

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Tebideutorexant

Tebideutorexant 構造式

CAS 番号 : 1637681-55-0

容量 価格（税別） 在庫状況 数量
1 mg $320 お問い合わせ 2-4 weeks 2-4 weeks 2-4 weeks 2-4 weeks
5 mg $780 お問い合わせ 2-4 weeks 2-4 weeks 2-4 weeks 2-4 weeks
10 mg $1250 お問い合わせ 2-4 weeks 2-4 weeks 2-4 weeks 2-4 weeks
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Tebideutorexant 関連抗体

Top Publications Citing Use of Products

Orexin Receptor (OX Receptor) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
OX2 Receptor OX1 Receptor

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製品説明

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.

Cellular Effect
Cell Line Type Value Description References
Vero C1008 IC50
>2.0 × 105 41
Compound: COVC-2283598831
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
10.6019/CHEMBL4651402
体外実験

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 関連抗体
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
体内実験

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.
分子量

460.42

分子式

C23H16D2F4N4O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
純度とドキュメンテーション
参考文献
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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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