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.
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- Pureza: 98.25%
- No. CAS: 1849603-79-7
- Fòrmula: C27H34N4O2
- Peso molecular:446.58
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Almacenamiento: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]
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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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Actividad biológica
Descripciòn
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.
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.
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Animal Model:C57BL/6J (male and female, 8-12 weeks old)[1]
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Dosage:12 mg/kg/10 µg (22 nmol); 1 µg
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Administration:i.p./i.t.; single dose
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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.
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Animal Model:Sprague Dawley (male and female, 8-12 weeks old)[1]
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Dosage:20 µg
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Administration:i.t.; single dose
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Result:Increased paw withdrawal threshold at 1, 2, 3, and 5 h post-injection.
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Animal Model:C57BL/6J (male and female, 8-12 weeks old, plantar incision model/tibial fracture model)[1]
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Dosage:12 mg/kg
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Administration:i.p.; single dose; administered immediately post-surgery/ single dose; administered 3 days post-surgery
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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.
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Animal Model:C57BL/6J (male and female, 8-12 weeks old, spared nerve injury model)[1]
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Dosage:12 mg/kg (single dose); 12 mg/kg (daily dosing)/10 µg (i.t.); 2 µg (intra-ganglionic)
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Administration:i.p./i.t.; single dose, administered 7 days post-surgery; daily for 5 consecutive days, starting 26 days post-surgery
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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.
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Animal Model:C57BL/6J (male and female, 8-12 weeks old, formalin model/complete Freund’s adjuvant model)[1]
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Dosage:12 mg/kg
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Administration:i.p.; single dose; administered with formalin injection/administered 1 day post-CFA
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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.
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Animal Model:CD-1 IGS (male and female, 8-12 weeks old, streptozotocin model)[1]
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Dosage:12 mg/kg
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Administration:i.p.; single dose; administered post-STZ-induced hyperglycemia
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Result:Increased PWT.
Reduced cold pain response duration.
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Animal Model:C57BL/6J (male and female, 8-12 weeks old)[1]
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Dosage:12 mg/kg (CPP test; withdrawal model); 30 mg/kg (CPP test)
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Administration:i.p.; single dose
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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
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No. CAS 1849603-79-7
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Appearance Solid
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Peso molecular 446.58
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Fòrmula C27H34N4O2
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Color Light yellow to yellow
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SMILES
OCCN(C)C1=CC2=C(N=C(C3(CC3)C)N=C2N4CCC(CC4)C5=C(OC)C=CC=C5)C=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 6 months -20°C 1 month
Solvente y solubilidad
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:
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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 (285 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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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