OX Receptor
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
OX Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7585 |
SB-334867SB-334867 is a selective orexin-1 (OX1) receptor antagonist. |
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| S1545 |
SB408124SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
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| S6726New |
MK1064MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM. |
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| S2160 |
Almorexant HClAlmorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3. |
(C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. ****P<0.0001; ***P<0.001; *P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).
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| S6717 |
TCS-OX2-29TCX-OX2-29 is a OX2R antagonist (pKi = 7.5) that exhibits >250-fold selectivity for hOX2R compared with hOX1R (IC50s = 40 nM and >10,000 nM, respectively). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7585 |
SB-334867SB-334867 is a selective orexin-1 (OX1) receptor antagonist. |
||
| S1545 |
SB408124SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
||
| S6726New |
MK1064MK1064 is a selective orexin 2 receptor antagonist (2-SORA) with an IC50 of 18 nM. |
||
| S2160 |
Almorexant HClAlmorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3. |
(C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. ****P<0.0001; ***P<0.001; *P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).
|
|
| S6717 |
TCS-OX2-29TCX-OX2-29 is a OX2R antagonist (pKi = 7.5) that exhibits >250-fold selectivity for hOX2R compared with hOX1R (IC50s = 40 nM and >10,000 nM, respectively). |
