2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel MAPK/ERK Pathway Stem Cell/Wnt
  3. Neurotensin Receptor Arrestin iGluR ERK Sodium Channel
  4. SBI-810

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.

SBI-810

SBI-810 Chemical Structure

CAS No. : 1849603-79-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SBI-810:

SBI-810 Related Antibodies

Top Publications Citing Use of Products

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AMPA Receptor NMDA Receptor Kainate Receptor

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ERK ERK1 ERK2 ERK5 ERK8

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Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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.

SBI-810 Related Antibodies
In Vivo

SBI-810 (12 mg/kg/10 µg~22 nmol); 1 µg; i.p./i.t.; single dose) 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) 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.
Molecular Weight

446.58

Formula

C27H34N4O2
CAS No.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2392 mL 11.1962 mL 22.3924 mL
5 mM 0.4478 mL 2.2392 mL 4.4785 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

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.

  • Protocol 1

    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.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 1.25 mg/mL (2.80 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    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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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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SBI-810 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SBI-8101849603-79-7SBI810SBI 810Neurotensin ReceptorArrestiniGluRERKSodium ChannelIonotropic glutamate receptorsExtracellular signal regulated kinasesNa channelsNa+ channelsNTSR1 modulatorblood-brain barrier-permeableHEK293T cellsDRG neuronsPhysiological acute painPostoperative painNeuropathic painInflammatory painDiabetic neuropathic painOpioid-induced reward and withdrawal
Inhibitorinhibitorinhibit

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