Cat. No.: HY-164795A

SBI-810 hydrochloride

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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.

For research use only. We do not sell to patients.

Purity: 99.55%
CAS No.: 2772746-58-2
Formula: C₂₇H₃₅ClN₄O₂
Molecular Weight:483.05

Storage:

4°C, sealed storage, away from moisture

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

SBI-810 hydrochloride Chemical Structure

CAS No.: 2772746-58-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Neurotensin Receptor Isoforms :

NTR1
NTR2

All Arrestin Isoforms :

All iGluR Isoforms :

All ERK Isoforms :

All Sodium Channel Isoforms :

In Vitro

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.

In Vivo

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.

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.

Chemical Information

CAS No. 2772746-58-2
Appearance Solid
Molecular Weight 483.05
Formula C₂₇H₃₅ClN₄O₂
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.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0702 mL

10.3509 mL

20.7018 mL

5 mM

0.4140 mL

2.0702 mL

4.1404 mL

10 mM

0.2070 mL

1.0351 mL

2.0702 mL

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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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SBI-810 hydrochloride

GPCR/G Protein Compound Library

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All Neurotensin Receptor Isoforms

All Arrestin Isoforms

All iGluR Isoforms

All ERK Isoforms

All Sodium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SBI-810 hydrochloride Related Classifications

HY-164795A Related Classifications