SB-334867 free base
Based on 14 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- No. CAS: 792173-99-0
- Fòrmula: C17H13N5O2
- Peso molecular:319.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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
Publications Citing Use of MedChemExpress (MCE) SB-334867 free base
More- J Neuroinflammation. 2024 May 17;21(1):131. [Abstract]
- Curr Biol. 2026 Aug 3;36(15):3767-3782.e6.
- Drug Des Devel Ther. 2022 Jul 5;16:2145-2160. [Abstract]
- Eur J Pharmacol. 2026 Feb 15:1015:178566. [Abstract]
- Exp Neurol. 2025 Nov:393:115378. [Abstract]
- J Inflamm Res. 2021 May 18:14:2007-2017. [Abstract]
- Brain Res Bull. 2023 Sep:201:110712. [Abstract]
- Front Neurosci. 2016 Jul 26:10:355. [Abstract]
- Brain Res. 2025 Nov 27:1872:150081. [Abstract]
- Neurogastroenterol Motil. 2026 Jul;38(7):e70389.
- Fundam Clin Pharmacol. 2026 May;40(3):e70091. [Abstract]
- Addict Biol. 2026 Jul;31(7):e70173. [Abstract]
- Biomed Pharmacother. 2021 Jul:139:111649. [Abstract]
- Research Square Preprint. 2021 Jan.
Customer Validation & Images
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Cell Proliferation/Viability Assay
Ver todos los productos específicos de isoformas Orexin Receptor (OX Receptor)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
OX1 Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
OX2 () |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
40 nM
Compound: SB-334867
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Antagonist activity at OX1 receptor expressed in CHO cells assessed as inhibition of OXA-stimulated intracellular calcium mobilization after 30 mins by FLIPR assay
Antagonist activity at OX1 receptor expressed in CHO cells assessed as inhibition of OXA-stimulated intracellular calcium mobilization after 30 mins by FLIPR assay
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[PMID: 22617492] |
In Vitro
SB-334867 (100 pM– 10 μM) inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses in a concentration-dependent manner, with apparent pKb values of 7.27±0.04 and 7.23±0.03, but has no effect on the calcium response elicited by UTP (3 μM), which activates an endogenous purinergic receptor in CHO-OX1 and CHO-OX2 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss mice[2]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection
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Result:Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice.
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Animal Model:C57BL/6J Mice[3]
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Dosage:3, 10 and 30 mg/kg
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Administration:Intraperitoneal injection
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Result:Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.
Chemical Information
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No. CAS 792173-99-0
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Appearance Solid
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Peso molecular 319.32
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Fòrmula C17H13N5O2
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Color White to off-white
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SMILES
O=C(NC1=CC(OC(C)=N2)=C2C=C1)NC3=CC=NC4=CC=CN=C43
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Synonyms
SB334867A free base
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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 (14)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
2024 May 17;21(1):131. PMID: 38760784 -
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Drug Des Devel Ther
Orexin-A Reverse Bone Mass Loss Induced by Chronic Intermittent Hypoxia Through OX1R-Nrf2/HIF-1α Pathway. [Abstract]2022 Jul 5;16:2145-2160. PMID: 35818538 -
Eur J Pharmacol
Bombesin improves visceral hypersensitivity and colonic hyperpermeability via BB1 receptor-dependent multi-pathway mechanisms in a rat model of irritable bowel syndrome. [Abstract]2026 Feb 15:1015:178566. PMID: 41548687 -
Exp Neurol
Orexin A alleviates chronic cerebral hypoperfusion-induced neuroinflammation and cognitive dysfunction by inhibiting the NEK7/NLRP3 pathway. [Abstract]2025 Nov:393:115378. PMID: 40691984 -
J Inflamm Res
Orexin-A Attenuates Inflammatory Responses in Lipopolysaccharide-Induced Neural Stem Cells by Regulating NF-KB and Phosphorylation of MAPK/P38/Erk Pathways. [Abstract]2021 May 18:14:2007-2017. PMID: 34040413 -
Brain Res Bull
Lateral hypothalamic orexin neurons mediate electroacupuncture-induced anxiolytic effects in a rat model of post-traumatic stress disorder. [Abstract]2023 Sep:201:110712. PMID: 37481143 -
Front Neurosci
Evidence for a Role of Orexin/Hypocretin System in Vestibular Lesion-Induced Locomotor Abnormalities in Rats. [Abstract]2016 Jul 26:10:355. PMID: 27507932
SB-334867 free base purchased from MedChemExpress. Usage Cited in: Front Neurosci. 2016 Jul 26:10:355. [Abstract]
Effects of the orexin receptor type 1 (OX1R) antagonist SB334867 on the vestibular deficit syndrome after vestibular lesions induced by arsanilate (A) and IDPN (B) in rats.
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Brain Res
Sex differences in interactions between the muscarinic-1 and orexin-1 receptors on cognitive flexibility in rats. [Abstract]2025 Nov 27:1872:150081. PMID: 41317779 -
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Fundam Clin Pharmacol
Repurposing Cimetidine as a Therapeutic Candidate for Irritable Bowel Syndrome in a Rat Model. [Abstract]2026 May;40(3):e70091. PMID: 42083465 -
Addict Biol
The Orexin System Modulates Stress-Induced Alcohol Preference and Reinstatement in Adolescents: Bioinformatics and Experimental Evidence. [Abstract]2026 Jul;31(7):e70173. PMID: 42337660 -
Biomed Pharmacother
Phlorizin attenuates visceral hypersensitivity and colonic hyperpermeability in a rat model of irritable bowel syndrome. [Abstract]2021 Jul:139:111649. PMID: 33957565 -
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (156.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 6 mg/mL (18.79 mM; ultrasonic and adjust pH to 3 with HCl)
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)
In Vivo:
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: ≥ 2.5 mg/mL (7.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (7.83 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
In Vivo Dissolution Calculator
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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Porter RA, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. [Content Brief]
[2]. Łupina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms. [Content Brief]
[3]. Anderson RI, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33. [Content Brief]
[4]. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist.Br J Pharmacol. 2001 Mar;132(6):1179-82. [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 |
|---|---|---|---|---|---|
| 0.1 M HCl / DMSO | 1 mM | 3.1317 mL | 15.6583 mL | 31.3165 mL | 78.2914 mL |
| 5 mM | 0.6263 mL | 3.1317 mL | 6.2633 mL | 15.6583 mL | |
| 10 mM | 0.3132 mL | 1.5658 mL | 3.1317 mL | 7.8291 mL | |
| 15 mM | 0.2088 mL | 1.0439 mL | 2.0878 mL | 5.2194 mL | |
| DMSO | 20 mM | 0.1566 mL | 0.7829 mL | 1.5658 mL | 3.9146 mL |
| 25 mM | 0.1253 mL | 0.6263 mL | 1.2527 mL | 3.1317 mL | |
| 30 mM | 0.1044 mL | 0.5219 mL | 1.0439 mL | 2.6097 mL | |
| 40 mM | 0.0783 mL | 0.3915 mL | 0.7829 mL | 1.9573 mL | |
| 50 mM | 0.0626 mL | 0.3132 mL | 0.6263 mL | 1.5658 mL | |
| 60 mM | 0.0522 mL | 0.2610 mL | 0.5219 mL | 1.3049 mL | |
| 80 mM | 0.0391 mL | 0.1957 mL | 0.3915 mL | 0.9786 mL | |
| 100 mM | 0.0313 mL | 0.1566 mL | 0.3132 mL | 0.7829 mL |
SB-334867 free base Related Classifications
HY-10895A Related Classifications
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