SBI-810 hydrochloride 

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^[1][2].

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 (12 mg/kg/10 µg~22 nmol); 1 µg; i.p./i.t.; single dose) hydrochloride exerts potent, NTSR1- and βarr2-dependent spinal analgesic effects in naive C57BL/6J mice, and alleviates physiological acute mechanical and thermal pain^[1].
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.

483.05

C₂₇H₃₅ClN₄O₂

2772746-58-2

Solid

Light yellow to yellow

OCCN(C)C1=CC2=C(N=C(C3(CC3)C)N=C2N4CCC(CC4)C5=C(OC)C=CC=C5)C=C1.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 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.

• [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]