| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
SRI-37330 HCl targets thioredoxin-interacting protein (TXNIP), an endogenous inhibitor of the antioxidant protein thioredoxin, involved in glucose metabolism and oxidative stress regulation.
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| ln Vitro |
In INS-1 cells, SRI-37330 HCl inhibits TXNIP expression with an IC50 of 0.64 microM. Its treatment inhibits glucagon secretion and function, decreases hepatic glucose production, and reverses hepatic steatosis in cellular models.
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| ln Vivo |
In rodent models of type 2 diabetes, oral administration of SRI-37330 HCl (doses ranging from 10-50 mg/kg) suppresses glucagon secretion, reduces blood glucose levels, improves insulin sensitivity, and reverses hepatic steatosis.
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| Enzyme Assay |
Detailed cell-free enzyme binding protocols are not standard as TXNIP is not an enzyme. A standard protocol would involve incubating purified TXNIP protein with varying concentrations of SRI-37330 HCl in binding buffer, followed by surface plasmon resonance or isothermal titration calorimetry to determine binding affinity (KD) and kinetics.
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| Cell Assay |
INS-1 cells are seeded in 96-well plates and treated with serial dilutions of SRI-37330 HCl (0.1-100 uM) for 24-48 hours. TXNIP mRNA expression is quantified by qRT-PCR, and protein expression is assessed by Western blot. Glucagon secretion is measured by ELISA following low glucose stimulation.
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| Animal Protocol |
Mice with diet-induced or genetically induced type 2 diabetes are orally administered SRI-37330 HCl (10-50 mg/kg) daily for 2-4 weeks. Blood glucose levels are measured weekly, and glucose tolerance tests are performed. Liver and pancreatic tissues are harvested for histological analysis and TXNIP expression quantification.
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| ADME/Pharmacokinetics |
Following oral administration in rodents, SRI-37330 HCl reaches peak plasma concentrations within 2-4 hours, with a terminal half-life of approximately 4-6 hours. Oral bioavailability is moderate to high (>50%), with distribution to liver and pancreas.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies in rodents at therapeutic doses (≤50 mg/kg) show a manageable safety profile without major adverse effects on body weight or major organ function. Higher doses may cause mild gastrointestinal disturbances. Standard safety precautions for oral administration in animal studies apply.
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| References | |
| Additional Infomation |
This compound is an investigational antidiabetic drug candidate, not yet approved for clinical use. It is provided as the hydrochloride salt for improved solubility. Purity ≥98%; molecular formula: C16H19F3N4O2S·HCl; molecular weight: 424.87.
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| Molecular Formula |
C16H20CLF3N4O2S
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|---|---|
| Molecular Weight |
424.87
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| Exact Mass |
424.094
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| CAS # |
2322245-49-6
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| Related CAS # |
SRI-37330;2322245-42-9
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| PubChem CID |
153319520
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
581
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(CCCN(C2=NC=NC3C2=CC(=CC=3)C(F)(F)F)C1)CNS(=O)(C)=O.Cl
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| InChi Key |
SIWGSSRKYJTJTF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19F3N4O2S.ClH/c1-26(24,25)22-8-11-3-2-6-23(9-11)15-13-7-12(16(17,18)19)4-5-14(13)20-10-21-15;/h4-5,7,10-11,22H,2-3,6,8-9H2,1H3;1H
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| Chemical Name |
N-[[1-[6-(trifluoromethyl)quinazolin-4-yl]piperidin-3-yl]methyl]methanesulfonamide;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) |
H2O : ~100 mg/mL (~235.37 mM)
DMSO : ~62.5 mg/mL (~147.10 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 | 2.3537 mL | 11.7683 mL | 23.5366 mL | |
| 5 mM | 0.4707 mL | 2.3537 mL | 4.7073 mL | |
| 10 mM | 0.2354 mL | 1.1768 mL | 2.3537 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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