SBI-810 hydrochloride
Based on 1 Customer Validation
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride 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 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.
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- Pureté: 99.55%
- CAS No.: 2772746-58-2
- Formule: C27H35ClN4O2
- Masse moléculaire:483.05
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
SBI-810 (10 min) hydrochloride 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) hydrochloride 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.
SBI-810 (20 µg; i.t.; single dose) hydrochloride exerts potent analgesic effects on physiological acute mechanical pain in naive Sprague Dawley rats[1].
SBI-810 (12 mg/kg; i.p.; single dose) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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.
Chemical Information
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CAS No. 2772746-58-2
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Appearance Solid
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Masse moléculaire 483.05
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Formule C27H35ClN4O2
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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.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 12.5 mg/mL (25.88 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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 (sealed storage, away from moisture). 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 | 2.0702 mL | 10.3509 mL | 20.7018 mL | 51.7545 mL |
| 5 mM | 0.4140 mL | 2.0702 mL | 4.1404 mL | 10.3509 mL | |
| 10 mM | 0.2070 mL | 1.0351 mL | 2.0702 mL | 5.1754 mL | |
| 15 mM | 0.1380 mL | 0.6901 mL | 1.3801 mL | 3.4503 mL | |
| 20 mM | 0.1035 mL | 0.5175 mL | 1.0351 mL | 2.5877 mL | |
| 25 mM | 0.0828 mL | 0.4140 mL | 0.8281 mL | 2.0702 mL |
SBI-810 hydrochloride Related Classifications
HY-164795A Related Classifications
Powered by Bioz
- SBI-810
- 2772746-58-2
- 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