| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SBI-810 hydrochloride targets the neurotensin receptor 1 (NTSR1), a class A G protein-coupled receptor (GPCR) activated by neurotensin (NT). It acts as a beta-arrestin-biased, functionally selective allosteric modulator, altering NTSR1-mediated G protein signaling in a G protein-specific manner. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, while remaining permissive toward NTSR1-mediated activation of GoA and G12. This biased modulation allows NTSR1 to activate specific signaling pathways, providing analgesic effects through both peripheral and central mechanisms.
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| ln Vitro |
In vitro, SBI-810 hydrochloride (0.1-100 uM) modulates NTSR1 G protein signaling in a G protein-specific manner. It fully antagonizes NT-induced Gq activation, inhibiting the production of inositol phosphates and calcium mobilization, and partially antagonizes NT-induced Gi1 activation. Unlike unbiased antagonists, it allows NTSR1 to activate GoA and G12 pathways. The compound does not completely block all NTSR1 signaling, preserving certain G protein-mediated responses while inhibiting others, which contributes to its biased agonism profile. It has a purity of ≥98%.
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| ln Vivo |
In vivo, SBI-810 hydrochloride produces analgesic effects through both peripheral and central mechanisms. By blocking NT-induced Gq activation while preserving GoA/G12 signaling, it mediates pain relief without the side effects associated with complete NTSR1 blockade. It has been studied in preclinical models for its potential in pain management. The compound is a research-grade chemical and is not an approved drug.
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| Enzyme Assay |
For in vitro NTSR1 binding studies, a radioligand binding assay can be used. Membranes from CHO cells expressing human NTSR1 are incubated with [3H]-neurotensin (0.1-1 nM) and varying concentrations of SBI-810 hydrochloride (0.1-1000 nM) in binding buffer (50 mM Tris-HCl pH 7.4, 1 mM EDTA, 0.1% BSA) at 25degC for 60-90 min. Bound radioactivity is separated by filtration, and IC₅0 is calculated. For G protein activation, GTPgammaS binding assays are performed.
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| Cell Assay |
For functional studies, CHO-NTSR1 cells are seeded in 96-well black plates (2×10⁴ cells/well) and loaded with a calcium-sensitive dye (e.g., Fluo-4 AM, 2-5 uM) for 30-60 min. SBI-810 hydrochloride (0.1-100 uM) is added for 15-30 min, then neurotensin (1-100 nM) is added to stimulate Gq-mediated calcium flux. The EC₅0 for antagonism of Gq activation is calculated. For Gi1 activation, a cAMP assay is used: cells are treated with forskolin (10 uM) and neurotensin, and cAMP is measured by ELISA. SBI-810 hydrochloride partially antagonizes Gi1 activation.
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| Animal Protocol |
In vivo analgesic efficacy can be evaluated in a mouse model of pain. Male C57BL/6 mice (6-8 weeks old, n=10/group) are injected with formalin (2.5%, 20 uL) into the hind paw to induce nociception. SBI-810 hydrochloride is formulated in 10% DMSO + 5% Tween 80 + 85% saline and administered intraperitoneally (1-10 mg/kg) 30 min before formalin injection. Licking/biting time is recorded for 0-5 min (acute phase) and 15-45 min (tonic phase). The compound reduces licking time, indicating analgesic activity. For central effects, intrathecal administration can be used.
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| ADME/Pharmacokinetics |
SBI-810 hydrochloride (MW 483.05) has good solubility in DMSO. For in vivo studies, it can be formulated in 10% DMSO + 5% Tween 80 + 85% saline or 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline. The compound is stored as a powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month. It should be stored in a sealed, protected environment, avoid exposure to moisture and light.
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| Toxicity/Toxicokinetics |
For SBI-810 hydrochloride, hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). Not for human consumption. For research use only.
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| References | |
| Additional Infomation |
SBI-810 hydrochloride (CAS# 2772746-58-2) is a research-grade beta-arrestin-biased, functionally selective allosteric modulator of the neurotensin receptor 1 (NTSR1). It is not an FDA-approved drug. It is used to study biased GPCR signaling, NTSR1 pharmacology, and as an analgesic tool in pain research. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C27H35CLN4O2
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|---|---|
| Molecular Weight |
483.05
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| Exact Mass |
482.245
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| CAS # |
2772746-58-2
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| Related CAS # |
SBI-810;1849603-79-7
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| PubChem CID |
155510650
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
636
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(CC1)C2=NC3=C(C=C(C=C3)N(C)CCO)C(=N2)N4CCC(CC4)C5=CC=CC=C5OC.Cl
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| InChi Key |
SZPSBVPAWFJWAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H34N4O2.ClH/c1-27(12-13-27)26-28-23-9-8-20(30(2)16-17-32)18-22(23)25(29-26)31-14-10-19(11-15-31)21-6-4-5-7-24(21)33-3;/h4-9,18-19,32H,10-17H2,1-3H3;1H
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| Chemical Name |
2-[[4-[4-(2-methoxyphenyl)piperidin-1-yl]-2-(1-methylcyclopropyl)quinazolin-6-yl]-methylamino]ethanol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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