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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
31 Results for "
OX1-R
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "OX1-R" in MCE Product Catalog:
12
12 Publications Verification
Synonyms: Hypocretin-1 (human, rat, mouse)
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12
12 Publications Verification
Cat. No.: HY-106224B
Pureté: 99.93%
Synonyms: Hypocretin-1 (human, rat, mouse) acetate
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12
12 Publications Verification
Cat. No.: HY-106224A
Pureté: 97.13%
Synonyms: Hypocretin-1 (human, rat, mouse) TFA
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2
2 Cited Publications
Cat. No.: HY-P1349
CAS No.: 202801-92-1
Synonyms: Rat orexin B; Orexin B (mouse)
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2
2 Cited Publications
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JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R [1] .
2
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1
1 Cited Publications
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YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models [1] .
1
1 Cited Publications
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YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models [1] .
Synonyms: ORN-0829; TS-142
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Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.
Cat. No.: HY-159835
CAS No.: 2460722-04-5
Synonyms: TAK-861
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Oveporexton (TAK-861) is an orally active and selective orexin receptor 2 (OX2R) agonist with an EC50 of 2.5 nM. Oveporexton exhibits 3000-fold selectivity for OX2R over OX1R. Oveporexton can be used for the study of hypersomnia disorders including narcolepsy [1] .
Synonyms: YZJ-1139
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Fazamorexant (YZJ-1139) is an orally active dual orexin receptor antagonist, with an IC50 of 32 nM against OX1R and an IC50 of 41 nM against OX2R. Fazamorexant prolongs total sleep time and improves sleep efficiency. Fazamorexant is applicable to related research on insomnia [1] .
Synonyms: ACT-539313
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Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder [1] .
Cat. No.: HY-147403S
CAS No.: 1637681-55-0
Synonyms: JNJ-61393215
Cat. No.: HY-162235
CAS No.: 1803557-42-7
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CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia [1].
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JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders [1] .
Cat. No.: HY-171032
CAS No.: 2923137-94-2
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(R)-YNT-3708 is a selective orexin 1 (OX1R) agonist, with an EC50 of 7.48 nM. (R)-YNT-3708 has antinociceptive effects [1].
Cat. No.: HY-178871
CAS No.: 1607428-33-0
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OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research [1].
Cat. No.: HY-171032B
CAS No.: 2923137-99-7
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YNT-3708 is an orexin receptor (OXR) agonist, with EC50 values of 14.6 nM and 277 nm for OX1R and OX2R, respectively [1].
Cat. No.: HY-171032A
CAS No.: 2923138-00-3
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(S)-YNT-3708, the S-enantiomer of YNT-3708, with low activity for OX1R and OX2R (EC50 = 3595 nM and 1661 nm, respectively) [1].
Cat. No.: HY-146517
CAS No.: 2251017-69-1
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Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1) [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
