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TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[2].
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
OX2R-IN-2 (compound 63c) is an agonist for orexin receptor type 2(OX2R) with EC50 of 339 nM. OX2R-IN-2 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
Firazorexton (TAK-994 free base) is an orally active, brain-permeable orexin type 2 receptor (OX2R) agonist. Firazorexton has the potential to improve narcolepsy like symptoms [2].
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia .
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 [2].
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.
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) .
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 [2].
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 [2].
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms [2] .
Firazorexton hydrate (TAK-994) is a potent, brain-penetrant, and orally active orexin type 2 receptor (OX2R) agonist (EC50: 19 nM). Firazorexton hydrate inhibits fragmentation of wakefulness and cataplexy-like episodes in mouse models of narcolepsy .
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 .
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation [2] .
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[2].
(2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton (HY-137440). Firazorexton is an orally active, brain-penetrating orexin type 2 receptor (OX2R) agonist that may improve narcolepsy-like symptoms ..
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation [2] .
Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
The CD200R1 protein is an inhibitory receptor that regulates key interactions by binding to the CD200/OX2 glycoprotein to limit inflammation by inhibiting TNF-α, interferon, and iNOS. Interestingly, CD200R1 displays comparable affinity and kinetics to the human herpesvirus 8 K14 viral CD200 homologue, reflecting its host CD200 interaction. CD200R1 Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived CD200R1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of CD200R1 Protein, Human (Biotinylated, HEK293, His-Avi) is 240 a.a., with molecular weight of 52-70 kDa.
The CD200R1 protein is an inhibitory receptor that regulates key interactions by binding to the CD200/OX2 glycoprotein to limit inflammation by inhibiting TNF-α, interferon, and iNOS. Interestingly, CD200R1 displays comparable affinity and kinetics to the human herpesvirus 8 K14 viral CD200 homologue, reflecting its host CD200 interaction. CD200R1 Protein, Human (HEK293, Fc) is the recombinant human-derived CD200R1 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of CD200R1 Protein, Human (HEK293, Fc) is 240 a.a., with molecular weight of 53.7 kDa.
The CD200R1 protein is an inhibitory receptor that regulates key interactions by binding to the CD200/OX2 glycoprotein to limit inflammation by inhibiting TNF-α, interferon, and iNOS. Interestingly, CD200R1 displays comparable affinity and kinetics to the human herpesvirus 8 K14 viral CD200 homologue, reflecting its host CD200 interaction. CD200R1 Protein, Human (HEK293, His-Avi) is the recombinant human-derived CD200R1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of CD200R1 Protein, Human (HEK293, His-Avi) is 240 a.a., with molecular weight of 52-70 kDa.
The CD200R1 protein is an inhibitory receptor that regulates key interactions by binding to the CD200/OX2 glycoprotein to limit inflammation by inhibiting TNF-α, interferon, and iNOS. Interestingly, CD200R1 displays comparable affinity and kinetics to the human herpesvirus 8 K14 viral CD200 homologue, reflecting its host CD200 interaction. CD200R1 Protein, Human (HEK293, His) is the recombinant human-derived CD200R1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CD200R1 Protein, Human (HEK293, His) is 240 a.a., with molecular weight of 50-80 kDa.
CD200R1 protein inhibits inflammatory responses by binding to CD200/OX2 cell surface glycoprotein and suppressing pro-inflammatory molecule expression. CD200R1 interacts with CD200 through their N-terminal Ig-like domains, providing a molecular mechanism for its role in regulating inflammation. CD200R1 Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived CD200R1 protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of CD200R1 Protein, Mouse (HEK293, His-Fc) is 213 a.a., with molecular weight of 90-100 kDa.
The CD200R1 protein is an inhibitory receptor that regulates key interactions by binding to the CD200/OX2 glycoprotein to limit inflammation by inhibiting TNF-α, interferon, and iNOS. Interestingly, CD200R1 displays comparable affinity and kinetics to the human herpesvirus 8 K14 viral CD200 homologue, reflecting its host CD200 interaction. CD200R1 Protein, Human (HEK293, His-Fc) is the recombinant human-derived CD200R1 protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of CD200R1 Protein, Human (HEK293, His-Fc) is 240 a.a., with molecular weight of 90-100 kDa.
CD200R1 protein inhibits inflammatory responses by binding to CD200/OX2 cell surface glycoprotein and suppressing pro-inflammatory molecule expression. CD200R1 interacts with CD200 through their N-terminal Ig-like domains, providing a molecular mechanism for its role in regulating inflammation. CD200R1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived CD200R1 protein, expressed by HEK293 , with C-His, C-6*His labeled tag. The total length of CD200R1 Protein, Mouse (HEK293, His) is 213 a.a., with molecular weight of 55-65 kDa.
CD200R1 Protein is an Ig superfamily transmembrane glycoprotein expressed on the surface of myeloid cells. CD200R1 Protein can also be induced in certain T-cell subsets. CD200R1 signaling inhibits the expression of proinflammatory molecules. CD200R1 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived CD200R1 protein, expressed by HEK293 , with C-His labeled tag. The total length of CD200R1 Protein, Cynomolgus (HEK293, His) is 221 a.a., with molecular weight of 43-75 KDa.
OX2R Protein, a nonselective, high-affinity receptor, functions as a key binding site for orexin-A and orexin-B neuropeptides. Its interaction with orexin-A leads to a significant increase in cytoplasmic Ca(2+) levels, indicating its involvement in cellular responses associated with neuropeptide activation. OX2R Protein, Human (Sf9, FLAG, His) is a recombinant protein dimer complex containing human-derived OX2R protein, expressed by Sf9 insect cells , with N-Flag, C-10*His labeled tag. OX2R Protein, Human (Sf9, FLAG, His), has molecular weight of 64.6 kDa.
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