| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Insulin Receptor (IR), specifically the IR-A and IR-B isoforms. In scintillation proximity assay (SPA), it shows IC50 values of 0.048 nM (HIR-A), 0.027 nM (HIR-B), and 630 nM (human IGF-1 receptor, HIGF-IR). It also binds rat IR (IC50=0.056 nM) and pig IR (IC50=0.084 nM) in PEG-assay.
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| ln Vitro |
In the PEG-assay, S961 also demonstrates strong affinity for Rat IR and Pig IR, with IC50s of 0.056 nM and 0.084 nM, respectively[1].
In vitro, S961 acetate exhibits sub-nanomolar antagonistic activity against insulin receptor with potent inhibition of insulin-induced receptor autophosphorylation and downstream signaling. The peptide effectively blocks insulin-stimulated glucose uptake in cell-based assays. In SPA and PEG binding assays, S961 demonstrates exceptional selectivity for IR over IGF-1R by over 10,000-fold. |
| ln Vivo |
In vivo, S961 acetate administration induces hyperglycemia in rodents by blocking insulin receptor signaling. This compound is extensively used to create pharmacologically induced insulin resistance and diabetic models in experimental animals via subcutaneous infusion or repeated injections. It elevates blood glucose levels and impairs glucose tolerance, serving as a valuable tool for studying type 2 diabetes and metabolic syndrome.
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| Enzyme Assay |
SPA-assay protocol: Membrane preparations of HIR-A, HIR-B, or HIGF-IR expressing cells are incubated with a fixed concentration of 125I-labeled insulin (approximately 0.1 nM) in 96-well plates containing SPA beads. Increasing concentrations of S961 acetate are added and the mixture is incubated for 16 hours at room temperature. Bound radioactivity is measured using a scintillation counter. Non-specific binding is determined in the presence of excess unlabeled insulin (1 uM). IC50 values are calculated by non-linear regression analysis.
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| Cell Assay |
In vitro cell-based assay protocol: Cells expressing insulin receptors (e.g., CHO-IR or 3T3-L1 adipocytes) are serum-starved overnight. After pre-incubation with S961 acetate (0-100 nM) for 30 min, cells are stimulated with insulin (1-10 nM) for 10 min. Receptor autophosphorylation is measured by immunoblotting with anti-phosphotyrosine antibodies. Alternatively, glucose uptake is measured using 2-deoxy-D-[3H]glucose. IC50 is determined by quantifying downstream Akt phosphorylation via ELISA.
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| Animal Protocol |
In vivo animal assay protocol: Male C57BL/6 mice are fasted overnight (12-16 hours) before the experiment. S961 acetate is dissolved in sterile saline and administered via subcutaneous injection at doses of 0.1-10 mg/kg or continuous subcutaneous infusion via osmotic minipump at 0.1-1 nmol/kg/min. Blood glucose levels are measured at baseline and at 30, 60, 90, and 120 min post-administration using a glucometer. For glucose tolerance tests, mice are challenged with glucose (1-2 g/kg, i.p.) 30 min after S961 treatment.
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| ADME/Pharmacokinetics |
Limited PK data are available for S961 acetate as a research peptide. As a large peptide (MW ~4800), it is expected to have low oral bioavailability, short plasma half-life due to rapid proteolytic degradation, primarily renal clearance for smaller peptide fragments, and minimal distribution across the blood-brain barrier under normal conditions. Typical subcutaneous administration yields Tmax around 1-2 hours.
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| Toxicity/Toxicokinetics |
Limited toxicological data available for S961 acetate in research settings. At standard research doses (0.1-10 mg/kg in rodents), acute toxicity is not generally reported, though sustained hyperglycemia from insulin receptor blockade can lead to metabolic disturbances, dehydration, and weight loss in longer-term studies. For acute exposure, the compound may cause local injection site reactions. No formal mutagenicity, carcinogenicity, or reproductive toxicity studies have been published.
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| References | |
| Additional Infomation |
S961 acetate is strictly a research tool compound and has not entered clinical trials or received regulatory approval for human therapeutic use. Its primary application is in academic and pharmaceutical research to study insulin receptor function, insulin resistance mechanisms, and metabolic disorders, serving as a pharmacological tool to mimic pathological states of insulin resistance and hyperglycemia in preclinical models.
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| Molecular Formula |
C213H301N55O72S2
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|---|---|
| Molecular Weight |
4864.18
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| Related CAS # |
S961;1083433-49-1;S961 TFA
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| Appearance |
White to off-white solid powder
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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) |
DMSO :~12.5 mg/mL (~2.57 mM)
H2O :~1.79 mg/mL (~0.37 mM) |
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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 | 0.2056 mL | 1.0279 mL | 2.0558 mL | |
| 5 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | |
| 10 mM | 0.0206 mL | 0.1028 mL | 0.2056 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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