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Orexinreceptor antagonist 4 is potent and selective orexin 2 receptor(OX2R) antagonist with an IC50 of 4.27 nM. Orexinreceptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1) .
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexinreceptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptorsOX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation .
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor(OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor(OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
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 .
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 .
OXA(17-33) is a potent and selective orexin-1 receptor(OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R .
OXA(17-33) TFA is a potent and selective orexin-1 receptor(OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
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 .
SB-408124 Hydrochloride is a selective non-peptide orexinreceptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor .
SB-674042 is a potent and selective non-peptide orexinOX1receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2receptors with IC50 values of 3.76 nM and 531 nM, respectively .
TCS 1102 is a potent, dual orexinreceptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats .
OX2R-IN-2 (compound 63c) is an agonist for orexinreceptor 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
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 .
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 .
EMPA is a high-affinity, reversible and selective orexinOX2receptor antagonist. [ 3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively .
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexinreceptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexinreceptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
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 .
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 .
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 .
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 .
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 .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptorOX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
Danavorexton (TAK-925) is an orexinreceptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
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 .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptorOX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
(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 orexinreceptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptorsOX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation .
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor(OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor(OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM) .
OXA(17-33) is a potent and selective orexin-1 receptor(OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R .
OXA(17-33) TFA is a potent and selective orexin-1 receptor(OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM) .
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 .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptorOX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptorOX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
OX1R, a moderately selective excitatory receptor, binds orexin-A and orexin-B neuropeptides. Upon orexin-A binding, OX1R activates cellular events, elevating cytoplasmic Ca(2+) levels. This interaction positions OX1R as a mediator in orexin neuropeptide signaling, influencing intracellular calcium dynamics in response to orexin-A. OX1R Protein, Human (HEK293, FLAG, His) is the recombinant human-derived OX1R protein, expressed by HEK293 , with C-10*His, N-Flag labeled tag. ,
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.
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
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