SRI-011381 (C381)

Catalog No.S6654 Batch:S665403

Technical Data

Formula	C₂₀H₃₁N₃O
Molecular Weight	329.48	CAS No.	1629138-41-5
Solubility (25°C)*	In vitro	DMSO	69 mg/mL (209.42 mM)
		Ethanol	69 mg/mL (209.42 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

SRI-011381 (C381) is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.C381 physically targets the lysosome, promotes lysosomal acidification, increases breakdown of lysosomal cargo, and improves lysosome resilience to damage.

Targets

TGF-β ^[1]

In vitro

SRI-011381 partially reverses the effect of sodium ferulate (SF) on the expression of fibrosis-related proteins, by increasing TGF-β1, NALP3, collagen-1, and α-SMA expression.^[2]

In vivo

SRI-011381, a small-molecule agonist of TGFβ signaling, has no effect on outflow tract (OFT) expansion in zebrafish, suggesting that hyperactivation of TGFβ signaling is not sufficient to induce aneurysm.^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines pulmonary fibroblasts of silicosis mouse model Concentrations 10 µM Incubation Time -- Method The tissues are extracted in a sterile environment, rinsed in PBS 3 times, and then cut into 1-mm³ tissue blocks. After repeated digestion with 0.25% trypsin at 37 ℃, the histolysate is evenly spread in a 10-cm petri dish. A high-glucose medium containing 10% fetal bovine serum, penicillin, and streptomycin is added to the petri dish. The cells are cultured in an incubator, and the medium is exchanged every 2-3 days. When the cells reached 80-90% confluence, they are passaged according to the ratio of 1: 3, and the fifth passage cells are taken for experimental study. Pulmonary fibroblasts are identified using anti-vimentin antibody with fluorescent secondary antibodies under a fluorescence microscope. For in vitro experiments, a range of concentrations of SF solution (0.04, 0.1, 0.18 and 0.28 mg/mL) are prepared for the treatment of fibroblasts. A 10 μM SRI-011381 solution is used for the activation of TGF-β1 signaling.
Animal Study:^{^[3]}	Animal Models Zebrafish carrying ltbp3^fb28 and ltbp1^fb29 Dosages 500 µM Administration exposed

Cell Assay:^{^[2]}

Cell lines
pulmonary fibroblasts of silicosis mouse model
Concentrations
10 µM
Incubation Time
--
Method
The tissues are extracted in a sterile environment, rinsed in PBS 3 times, and then cut into 1-mm³ tissue blocks. After repeated digestion with 0.25% trypsin at 37 ℃, the histolysate is evenly spread in a 10-cm petri dish. A high-glucose medium containing 10% fetal bovine serum, penicillin, and streptomycin is added to the petri dish. The cells are cultured in an incubator, and the medium is exchanged every 2-3 days. When the cells reached 80-90% confluence, they are passaged according to the ratio of 1: 3, and the fifth passage cells are taken for experimental study. Pulmonary fibroblasts are identified using anti-vimentin antibody with fluorescent secondary antibodies under a fluorescence microscope. For in vitro experiments, a range of concentrations of SF solution (0.04, 0.1, 0.18 and 0.28 mg/mL) are prepared for the treatment of fibroblasts. A 10 μM SRI-011381 solution is used for the activation of TGF-β1 signaling.

Animal Study:^{^[3]}

Animal Models
Zebrafish carrying ltbp3^fb28 and ltbp1^fb29
Dosages
500 µM
Administration
exposed

References

[4] Vest RT, et al. Proc Natl Acad Sci U S A. 2022 Mar 15;119(11):e2121609119.

+ Expand

Selleck's SRI-011381 (C381) has been cited by 4 publications

Latent TGFβ binding proteins 1 and 3 protect the larval zebrafish outflow tract from aneurysmal dilatation [ Dis Model Mech, 2022, dmm.046979]	PubMed: 35098309
Cartilage Endplate Stem Cells Transdifferentiate Into Nucleus Pulposus Cells via Autocrine Exosomes [ Front Cell Dev Biol, 2021, 9:648201]	PubMed: 33748142
MicroRNA-210-5p alleviates cardiac fibrosis via targeting transforming growth factor-beta type I receptor in rats on high sodium chloride (NaCl)-based diet [ Eur J Pharmacol, 2021, 912:174587]	PubMed: 34678242
MMP11 promotes the proliferation and progression of breast cancer through stabilizing Smad2 protein [ Oncol Rep, 2021, 45(4)16]	PubMed: 33649832

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SHIPPING AND STORAGE
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