SB-674042
Based on 3 publication(s) in Google Scholar
SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively.
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- Pureza: 99.87%
- No. CAS: 483313-22-0
- Fòrmula: C24H21FN4O2S
- Peso molecular:448.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB-674042
MoreVer todos los productos específicos de isoformas Orexin Receptor (OX Receptor)
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Actividad biológica
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OX1 Receptor 3.76 nM (IC50) |
OX2 Receptor 531 nM (IC50) |
OX1 Receptor 1.1 nM (Ki) |
OX2 Receptor 129 nM (Ki) |
SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells[1].
SB-674042 (5 μM; 4 °C for 30 min, and 37 °C for 3 h) reduces the potency of CB1 receptor agonist (HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors[2].
SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)[4]
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Dosage:0.3 nM/0.3 μL
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Administration:Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
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Result:Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.
Chemical Information
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No. CAS 483313-22-0
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Appearance Solid
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Peso molecular 448.51
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Fòrmula C24H21FN4O2S
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Color White to off-white
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SMILES
FC1=C(C2=C(C(N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Neuropsychopharmacology
Selective orexin receptor cross-over treatment increases resilience and expression of neuroplastic signaling genes. [Abstract]2026 Jun 21. PMID: 42323509 -
Neuropharmacology
Contextual generalization of social stress learning is modulated by orexin receptors in basolateral amygdala. [Abstract]2022 Sep 1:215:109168. PMID: 35724928 -
bioRxiv
Prioritizing Neuroactive Ligands Using Motif-Guided Virtual Discovery and Zebrafish Profiling. [Abstract]2026 Jan 16:2026.01.15.699747. PMID: 41648545
Solvente y solubilidad
DMSO : 25 mg/mL (55.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Langmead CJ, et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6. [Content Brief]
[2]. Ellis J, et al. Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. J Biol Chem. 2006 Dec 15;281(50):38812-24. [Content Brief]
[3]. Chang X, et al. Orexin-A Stimulates Insulin Secretion Through the Activation of the OX1 Receptor and Mammalian Target of Rapamycin in Rat Insulinoma Cells. Pancreas. 2019 Apr;48(4):568-573. [Content Brief]
[4]. Yaeger JDW, et al. Orexin 1 Receptor Antagonism in the Basolateral Amygdala Shifts the Balance From Pro- to Antistress Signaling and Behavior. Biol Psychiatry. 2022 May 1;91(9):841-852. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2296 mL | 11.1480 mL | 22.2960 mL | 55.7401 mL |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4592 mL | 11.1480 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL | 5.5740 mL | |
| 15 mM | 0.1486 mL | 0.7432 mL | 1.4864 mL | 3.7160 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1148 mL | 2.7870 mL | |
| 25 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2296 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8580 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3935 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL |
SB-674042 Related Classifications
HY-10898 Related Classifications
Powered by Bioz
- SB-674042
- 483313-22-0
- SB674042
- SB 674042
- Orexin Receptor (OX Receptor)
- hypocretin
- [3 H]SB-674042
- SB-334867
- SB-408124
- SB-410220
- radioligand binding
- CHO
- Chinese hamster ovary cells
- FLIPR
- fluorometric imaging plate reader
- SPA
- scintillation proximity assay
- WGA-PVT
- wheatgerm-agglutinin polyvinyltoluene
- Inhibitor
- inhibitor
- inhibit