SRI-011381 |
| رقم الكتالوجGC45831 |
SRI-011381 هو ناهض إشارات TGF-نشط عن طريق الفم ، يعرض تأثيرات اعصاب
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1629138-41-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
SRI-011381 is an orally active activator of the transforming growth factor β (TGF-β) signaling pathway with neuroprotective effects[1]. TGF-β is a multi-effect cytokine that regulates cell growth and differentiation, apoptosis, cell motility, extracellular matrix production, angiogenesis, and cellular immune responses[2]. SRI-011381 has important application value in the study of tissue repair and fibrotic diseases[3].
In vitro, SRI-011381 (10μM) treatment of mouse lung fibroblasts for 48h promoted cell proliferation and increased the expression of intracellular TGF-β1, neutrophil alkaline phosphatase 3 (NALP3), collagen-1, and α-smooth muscle actin (α-SMA) proteins[4].
In vivo, SRI-011381 (30mg/kg) was intraperitoneally injected into rats with heart failure (HF) model, which reversed the protective effect of SMOC2 knockdown (sh-SMOC2) against HF, aggravated cardiac injury and fibrosis, and reversed the regulation of p-Smad3, p62, LC3-II/I, and Beclin-1 by sh-SMOC2[5]. SRI-011381 (30mg/kg) was intraperitoneally injected into YAPGFAP-CKO mice with experimental autoimmune encephalomyelitis (EAE), which inhibited inflammatory infiltration, alleviated neuronal loss, and partially rescued the optic nerve and retinal defects of mice[6].
References:
[1] Wang J, Yang L, Mei J, et al. Knockdown of notch suppresses epithelial-mesenchymal transition and induces angiogenesis in oral submucous fibrosis by regulating TGF-β1[J]. Biochemical Genetics, 2024, 62(2): 1055-1069.
[2] Moustakas A, Pardali K, Gaal A, et al. Mechanisms of TGF-β signaling in regulation of cell growth and differentiation[J]. Immunology letters, 2002, 82(1-2): 85-91.
[3] Yao C, Zhou X, Weng W, et al. Aligned nanofiber nerve conduits inhibit alpha smooth muscle actin expression and collagen proliferation by suppressing TGF-β1/SMAD signaling in traumatic neuromas[J]. Experimental and Therapeutic Medicine, 2021, 22(6): 1414.
[4] Han J, Jia Y, Wang S, et al. The improvement effect of sodium ferulate on the formation of pulmonary fibrosis in silicosis mice through the neutrophil alkaline phosphatase 3 (NALP3)/transforming growth factor-β1 (TGF-β1)/α-smooth muscle actin (α-SMA) pathway[J]. Medical Science Monitor: International Medical Journal of Experimental and Clinical Research, 2021, 27: e927978-1.
[5] Ren Y, Wu Y, He W, et al. SMOC2 plays a role in heart failure via regulating TGF-β1/Smad3 pathway-mediated autophagy[J]. Open Medicine, 2023, 18(1): 20230752.
[6] Wu Q, Miao X, Zhang J, et al. Astrocytic YAP protects the optic nerve and retina in an experimental autoimmune encephalomyelitis model through TGF-β signaling[J]. Theranostics, 2021, 11(17): 8480.
| Cell experiment [1]: | |
Cell lines | Fibroblasts |
Preparation Method | Sodium ferulate (SF) solutions of different concentrations (0.04, 0.1, 0.18 and 0.28mg/mL) were prepared to treat fibroblasts for 48h. 10μM SRI-011381 solution was added to activate the TGF-β1 signaling pathway. The effect of SRI011381 on the viability of fibroblasts was detected by CCK8 assay. The effect of SRI-011381 on the expression of TGF-b1, neutrophil alkaline phosphatase 3 (NALP3), collagen-1, and alpha-smooth muscle actin (a-SMA) proteins was detected by western blot. |
Reaction Conditions | 10μM; 48h |
Applications | SRI-011381 promoted cell proliferation and increased the expression of intracellular TGF-β1, NALP3, collagen-1, and α-SMA proteins. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | To establish the rat models of Heart failure (HF), rats were adaptively fed for 1 week and fasted for 12h. The rats were intraperitoneally injected with 1.5% sodium pentobarbital (50mg/kg) for anesthesia. Then, the left coronary artery of rats was ligated at the position between the left atrial appendage and the pulmonary conus on a temperature-controlled heating pad. The abdomen was sutured in layers. Rats in the sham operation group underwent the same procedure but without the left coronary artery ligation. To further investigate the function of SMOC2 in HF development, lentivirus carrying sh-SMOC2 or short hairpin RNA negative control (sh-NC) was injected into the infarct area of HF rats immediately after induction of myocardial infarction. Therefore, rats were randomly assigned into four groups (n=6/group): sham operation (sham), HF rat model (HF), HF rat model treated with lentivirus carrying sh-NC (HF+sh-NC), and HF rat model treated with lentivirus carrying sh-SMOC2 (HF+sh-SMOC2). TGF-β agonist (SRI-011381, 30mg/kg daily) was intraperitoneally injected into rat model 5 days after lentivirus injection. After 4 weeks of injection, rats were sacrificed by cervical dislocation, and myocardial tissues were collected for subsequent assays. |
Dosage form | 30mg/kg; i.p. |
Applications | SRI-011381 reverses the protective effect of SMOC2 knockdown (sh-SMOC2) against heart failure (HF) and aggravates cardiac injury and fibrosis. SRI-011381 treatment reversed the effects of sh-SMOC2 on decreasing the levels of p-Smad3 and p62 and increasing LC3-II/I ratio and Beclin-1 levels in HF rats. |
References: | |
| Cas No. | 1629138-41-5 | SDF | |
| Canonical SMILES | O=C(NC1CCCCC1)N(CC2CCNCC2)CC3=CC=CC=C3 | ||
| Formula | C20H31N3O | M.Wt | 329.5 |
| الذوبان | DMF: 15mg/mL,DMSO: 20mg/mL,Ethanol: 25mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0349 mL | 15.1745 mL | 30.349 mL |
| 5 mM | 607 μL | 3.0349 mL | 6.0698 mL |
| 10 mM | 303.5 μL | 1.5175 mL | 3.0349 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *