SBI-810
Based on 1 Customer Validation
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.
For research use only. We do not sell to patients.
- Purity : 98.25%
- CAS No.: 1849603-79-7
- Formula: C27H34N4O2
- Molecular Weight:446.58
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vitro
SBI-810 (10 min) stimulates the recruitment of β-arrestin 2 to human NTSR1 in HEK293T cells, and antagonizes Gq activation induced by Neurotensin (NT) (HY-P0234)[1].
Bath-applied SBI-810 (5 μM, administered during recording) decreases the action potential firing frequency of DRG neurons, increases their rheobase, and inhibits neuronal excitability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
SBI-810 (20 µg; i.t.; single dose) exerts potent analgesic effects on physiological acute mechanical pain in naive Sprague Dawley rats[1].
SBI-810 (12 mg/kg; i.p.; single dose) potently inhibits pain in mouse plantar incision and tibial fracture post-surgical pain models[1].
SBI-810 (12 mg/kg/10 µg; i.p./i.t.; single dose, administered 7 days post-surgery) exerts potent, NTSR1- and βarr2-dependent analgesic effects in SNI model mice, alleviating neuropathic mechanical allodynia and cold allodynia[1].
SBI-810 (12 mg/kg; i.p.; single dose; administered concurrently with formalin injection) potently inhibits inflammatory hyperalgesia and mechanical allodynia, and reduces formalin-induced activation of nociceptors in DRG neurons in mouse formalin/CFA (HY-153808) inflammatory pain models[1].
SBI-810 (12 mg/kg; i.p.; single dose; administered post-STZ-induced hyperglycemia) potently alleviates mechanical pain and cold pain in mice with STZ (HY-13753)-induced diabetic neuropathic pain[1].
SBI-810 (12-30 mg/kg; i.p.; single dose) attenuates or abolishes morphine-induced CPP, and significantly reduces the cumulative withdrawal score induced by Naloxone (HY-17417A) in mice treated with escalating doses of morphine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (male and female, 8-12 weeks old)[1]
-
Dosage:12 mg/kg/10 µg (22 nmol); 1 µg
-
Administration:i.p./i.t.; single dose
-
Result:Increased the paw withdrawal threshold (PWT) in the von Frey test (peak effect occurs at 2–3 hours).
Prolonged the paw withdrawal latency in the hot plate test, Hargreaves test, and dry ice test.
Exhibited consistent analgesic effects in both male and female mice.
-
Animal Model:Sprague Dawley (male and female, 8-12 weeks old)[1]
-
Dosage:20 µg
-
Administration:i.t.; single dose
-
Result:Increased paw withdrawal threshold at 1, 2, 3, and 5 h post-injection.
-
Animal Model:C57BL/6J (male and female, 8-12 weeks old, plantar incision model/tibial fracture model)[1]
-
Dosage:12 mg/kg
-
Administration:i.p.; single dose; administered immediately post-surgery/ single dose; administered 3 days post-surgery
-
Result:Prevented incision-induced mechanical hyperalgesia.
Blocked incision-induced spontaneous pain.
Reduced facial expressions of pain.
Increased PWT (Prognostic Threat).
Reduced protective behavior scores.
Shortened the duration of cold pain response.
-
Animal Model:C57BL/6J (male and female, 8-12 weeks old, spared nerve injury model)[1]
-
Dosage:12 mg/kg (single dose); 12 mg/kg (daily dosing)/10 µg (i.t.); 2 µg (intra-ganglionic)
-
Administration:i.p./i.t.; single dose, administered 7 days post-surgery; daily for 5 consecutive days, starting 26 days post-surgery
-
Result:Increased PWT shortened the duration of the cold pain response.
Induced a significant conditioned place preference (CPP), indicating relief of persistent neuropathic pain.
Did not impair cognitive function in the new object recognition test.
-
Animal Model:C57BL/6J (male and female, 8-12 weeks old, formalin model/complete Freund’s adjuvant model)[1]
-
Dosage:12 mg/kg
-
Administration:i.p.; single dose; administered with formalin injection/administered 1 day post-CFA
-
Result:Shortened the duration of spontaneous pain responses.
Reduced pERK-positive DRG neurons by approximately 70%.
Increased paw withdrawal latency in Hargreaves test, increased PWT in von Frey test.
-
Animal Model:CD-1 IGS (male and female, 8-12 weeks old, streptozotocin model)[1]
-
Dosage:12 mg/kg
-
Administration:i.p.; single dose; administered post-STZ-induced hyperglycemia
-
Result:Increased PWT.
Reduced cold pain response duration.
-
Animal Model:C57BL/6J (male and female, 8-12 weeks old)[1]
-
Dosage:12 mg/kg (CPP test; withdrawal model); 30 mg/kg (CPP test)
-
Administration:i.p.; single dose
-
Result:Reduced morphine-induced CPP dose-dependently at 12 mg/kg, and eliminated morphine-induced CPP at 30 mg/kg.
Significantly reduced naloxone-induced cumulative withdrawal scores in mice treated with escalating morphine doses at 12 mg/kg.
Chemical Information
-
CAS No. 1849603-79-7
-
Appearance Solid
-
Molecular Weight 446.58
-
Formula C27H34N4O2
-
Color Light yellow to yellow
-
SMILES
OCCN(C)C1=CC2=C(N=C(C3(CC3)C)N=C2N4CCC(CC4)C5=C(OC)C=CC=C5)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (22.39 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1 mg/mL (2.24 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 1.25 mg/mL (2.80 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (22.39 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Synaptic current patch-clamp recording in brain slices
Whole-cell patch-clamp recording in acute brain slices measures membrane current from visually identified neurons while preserving part of the local synaptic circuit; in voltage clamp, postsynaptic currents are generated by synaptic receptor-channel activation and are recorded as inward or outward currents at a defined holding potential. Miniature synaptic currents are recorded during action-potential blockade with tetrodotoxin, whereas evoked synaptic currents are generated by pathway stimulation and isolated pharmacologically as EPSCs or IPSCs.
-
Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
-
Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
-
Acute brain-slice whole-cell patch-clamp recording
Acute brain-slice whole-cell patch-clamp recording measures membrane voltage or ionic current from visually targeted cells in living brain slices; after giga-seal formation, the membrane under the pipette is ruptured to provide low-resistance electrical access to the cell interior, enabling current-clamp analysis of excitability and voltage-clamp analysis of synaptic or membrane currents. Acute slices preserve local tissue architecture better than dissociated preparations and allow visually guided recording from defined brain regions or fluorescently labeled cells; however, whole-cell access also permits exchange between pipette solution and cytoplasm, so intracellular dialysis must be considered when interpreting signaling-dependent phenomena.
-
Cell-attached patch-clamp recording
Cell-attached patch-clamp recording measures ionic current through one or more ion channels in a small membrane patch that remains attached to an intact cell; the readout is a time-resolved current trace generated when channels in the sealed patch open and close under controlled pipette voltage or stimulus conditions. Classic applications include single acetylcholine receptor currents in frog skeletal muscle, single sodium-channel currents in cultured rat muscle cells, one-channel NMDA receptor recordings, and mechanically activated PIEZO-channel recordings. The method depends on forming a high-resistance pipette-membrane seal, commonly described as a gigaohm seal, which reduces leak and noise sufficiently to resolve picoampere-scale single-channel currents. In the cell-attached configuration, the patch membrane is not ruptured, so cytosolic composition is not directly dialyzed by the pipette solution.
-
Primary Dorsal Root Ganglion Sensory Neuron Culture
Primary dorsal root ganglion sensory neuron culture isolates DRG neuronal somata from rodent or human ganglia, dissociates tissue enzymatically and mechanically, and maintains post-mitotic sensory neurons in vitro for readouts such as neurite outgrowth, immunocytochemical marker expression, calcium imaging, electrophysiology, RNA/protein analysis, or neuropeptide release assays. The method reflects peripheral sensory neuron biology because DRG neurons are primary sensory neurons whose cell bodies reside in dorsal root ganglia and whose cultured dissociated cells can retain neuronal morphology, sensory-neuron marker expression, and stimulus-responsive properties depending on the downstream assay.
Purity & Documentation
-
Data Sheet (285 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
[1]. Guo R, et al. Arrestin-biased allosteric modulator of neurotensin receptor 1 alleviates acute and chronic pain. Cell. 2025;188(16):4332-4349.e21. [Content Brief]
[2]. Pottie E, et al. Pain management beyond opioids: a β-arrestin2-biased allosteric GPCR modulator opens new avenues for drug development. Signal Transduct Target Ther. 2025 Aug 27;10(1):264. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2392 mL | 11.1962 mL | 22.3924 mL | 55.9810 mL |
| 5 mM | 0.4478 mL | 2.2392 mL | 4.4785 mL | 11.1962 mL | |
| 10 mM | 0.2239 mL | 1.1196 mL | 2.2392 mL | 5.5981 mL | |
| 15 mM | 0.1493 mL | 0.7464 mL | 1.4928 mL | 3.7321 mL | |
| 20 mM | 0.1120 mL | 0.5598 mL | 1.1196 mL | 2.7991 mL |
SBI-810 Related Classifications
HY-164795 Related Classifications
Powered by Bioz
Keywords
- SBI-810
- 1849603-79-7
- SBI810
- SBI 810
- Neurotensin Receptor
- Arrestin
- iGluR
- ERK
- Sodium Channel
- NTSR1 modulator
- blood-brain barrier-permeable
- HEK293T cells
- DRG neurons
- Physiological acute pain
- Postoperative pain
- Neuropathic pain
- Inflammatory pain
- Diabetic neuropathic pain
- Opioid-induced reward and withdrawal
- Inhibitor
- inhibitor
- inhibit