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| 25mg |
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| Targets |
TGF-beta[1]; SRI-011381 targets the TGF-β signaling pathway as an agonist . It activates TGF-β/Smad‑dependent signaling by promoting the phosphorylation of Smad2 and Smad3 . The compound also activates the non‑Smad PI3K signaling pathway . In SBE‑luciferase bioluminescent reporter mice, SRI-011381 (30 mg/kg, i.p.) activates TGF‑β signaling in vivo .
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| ln Vitro |
SRI-011381 (10 μM) hydrochloride greatly boosts the expression of TGF-β1, NALP3, collagen-1, and α-SMA while also encouraging the growth of mice lung fibroblasts[1]. In stemness acquisition studies, SRI-011381 promotes sphere formation in NSTCs through the Prrx1/TGF‑β/smad signaling axis . It increases fibronectin expression in NIH‑3T3 cells stimulated by metformin . SRI-011381 (10 μM) abolishes the protective effect of saikosaponin A (SSA, 30 μM) on fibroblasts . In placental trophocytes with TGF‑β1 overexpression, SRI-011381 increases mRNA levels of Smad2 (2.58±0.22 vs. 1.00±0.13), Smad3 (2.27±0.24 vs. 1.00±0.15), and Smad4 (2.04±0.19 vs. 1.00±0.11) while decreasing E‑Cadherin mRNA levels (0.47±0.07 vs. 1.00±0.09) . The compound also enhances TGF‑β1 secretion, promotes angiogenesis through tubule formation assays, and increases migration of HUVECs as demonstrated by Transwell assays .
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| ln Vivo |
The deficiencies in the optic nerve and retina of YAPGFAP-CKO EAE mice are largely restored by SRI-011381 (30 mg/kg; ip; every 2 d; for 22 days) hydrochloride[2].
SRI-011381 (30 mg/kg, i.p.) activates TGF‑β signaling in SBE‑luciferase bioluminescent reporter mice . The compound (7 mg/kg, i.p., 2 weeks) reverses the beneficial effects of internal heat needle therapy in a rotator cuff injury rat model, as evidenced by shortened thermal withdrawal latency, decreased maximum tensile load, reduced expression of Scx and TnC, increased levels of IL‑1β, IL‑6, and TNF‑α, and elevated expression of TGF‑β1 and p‑Smad2/3 . SRI-011381 protects mice from kainic acid‑induced excitotoxicity and neurodegeneration . It reduces neurodegeneration in APP751SL Swedish transgenic mice . In an embryo damage model, SRI-011381 inhibits E‑Cadherin expression via Smad signaling pathway activation . |
| Enzyme Assay |
: Western blot analysis – treated cells are lysed, proteins resolved by electrophoresis, transferred to membranes, and probed with antibodies against TGF‑β1, p‑Smad2, p‑Smad3, and stemness markers (CD133, SOX2) to assess pathway activation . ELISA – cell culture supernatants are collected and analyzed for TGF‑β1 secretion levels using commercial ELISA kits to quantify pathway activation . Sphere formation assay – cells are cultured in ultra‑low attachment plates and the number and size of spheres are quantified to assess stemness acquisition . Tubule formation assay – HUVECs are plated on Matrigel and capillary‑like tube structures are visualized and quantified to assess angiogenesis .
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| Cell Assay |
Sphere formation assay – cells (NSTCs or GSCs) are treated with SRI-011381 and cultured under stemness‑promoting conditions; the number and size of spheres formed are quantified to evaluate the effect on stemness acquisition . Tubule formation assay – HUVECs are treated with conditioned medium from NSTCs or GSCs stimulated with SRI-011381 and plated on Matrigel; capillary‑like tube structures are visualized microscopically and quantified by measuring tube length and branch points . Transwell migration assay – HUVECs are seeded in the upper chamber of a Transwell insert, and conditioned medium from compound‑treated NSTCs or GSCs is placed in the lower chamber; after incubation, migrated cells on the lower surface of the membrane are stained and counted . Western blot analysis – treated cells are lysed in RIPA buffer, proteins separated by SDS‑PAGE, transferred to PVDF membranes, and probed with antibodies against TGF‑β1, p‑Smad2, p‑Smad3, Smad2, Smad3, CD133, and SOX2 to assess protein expression changes . ELISA – cell culture supernatants are collected and analyzed for TGF‑β1 secretion levels using commercial ELISA kits according to the manufacturer‘s protocol . Gene expression analysis (qPCR) – total RNA is extracted from treated cells, reverse transcribed to cDNA, and subjected to fluorescence quantitative PCR for detection of Smad2, Smad3, Smad4, PI3K, and E‑Cadherin mRNA levels .
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| Animal Protocol |
Animal/Disease Models: YAPGFAP-CKO mice bearing experimental autoimmune encephalomyelitis (EAE)[2]
Doses: 30 mg/kg Route of Administration: intraperitoneally (ip) injection; every 2 d; for 22 days Experimental Results: Dramatically inhibited inflammatory infiltration and relieved the loss of neurons in YAPGFAP-CKO EAE mice. Rotator cuff injury model in SD rats – Male SPF SD rats (8 weeks old, 200±20 g) are anesthetized with pentobarbital sodium. The supraspinatus tendon insertion at the greater tuberosity is exposed and transected approximately halfway to induce rotator cuff injury. SRI-011381 is administered intraperitoneally at 7 mg/kg for 2 weeks (once weekly). Therapeutic outcomes are assessed by thermal withdrawal latency (TWL), inflammatory cytokine levels (IL‑1β, IL‑6, TNF‑α) via ELISA, histopathological examination (HE staining), collagen fiber assessment (Masson staining), maximum tensile load biomechanical testing, and immunohistochemical staining of Scx and TnC . SBE‑luciferase bioluminescent reporter mice – SRI-011381 is administered intraperitoneally at 30 mg/kg, and TGF‑β signaling activation is measured via bioluminescence imaging . Neuroprotection studies – Mice are treated with kainic acid to induce excitotoxicity; SRI-011381 is administered and neuroprotective effects are assessed . Alzheimer‘s disease model (APP751SL Swedish transgenic mice) – SRI-011381 is administered and neurodegeneration reduction is evaluated . |
| ADME/Pharmacokinetics |
SRI-011381 is orally bioavailable with an oral bioavailability of approximately 50% in FBV mice . Following oral administration in FBV mice, SRI-011381 is rapidly absorbed . Solubility: DMSO: 125 mg/mL (379.39 mM) . For in vivo formulation, the compound can be prepared in 10% DMSO + 40% PEG300 + 5% Tween‑80 + 45% Saline at a concentration of 2 mg/mL (6.07 mM) with sonication recommended . The hydrochloride salt form (SRI-011381 hydrochloride) has a molecular weight of 365.94 and CAS number 2070014-88-7 . The free base form has molecular weight 329.48 and CAS number 1629138-41-5 .
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| Toxicity/Toxicokinetics |
In FBV mice treated with SRI-011381 (10‑75 mg/kg, oral, 14 days), significant changes in hematological endpoints were observed, most notably decreases in red blood cells, hematocrit, and hemoglobin . According to Safety Data Sheets, SRI-011381 hydrochloride is classified as toxic and contains a pharmaceutically active ingredient; handling should only be performed by personnel trained in handling potent active pharmaceutical ingredients . It is a moderate to severe irritant to the skin and eyes . Potential toxicity includes: very toxic if swallowed (R28), irritating to skin (R38), risk of serious damage to eyes (R41), toxic with danger of serious damage to health by prolonged exposure (R48), possible risk of impaired fertility (R62), and possible risk of harm to the unborn child (R63) . The substance is not listed as a carcinogen by NTP, IARC, OSHA, or ACGIH . Upon combustion, may emit irritant fumes . The product is for research use only and not for human or veterinary use .
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| References |
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| Additional Infomation |
SRI-011381 (CAS: 1629138-41-5 for free base; 2070014-88-7 for hydrochloride salt) has the molecular formula C20H31N3O and molecular weight 329.48 (free base) . The chemical name is Urea, N‘‑cyclohexyl‑N‑(phenylmethyl)‑N‑(4‑piperidinylmethyl)‑, hydrochloride (1:1) for the salt form . Smiles: O=C(NC1CCCCC1)N(CC1CCNCC1)Cc1ccccc1 . The compound is stable when stored as directed; protect from light and heat . Storage recommendations: powder at -20°C for up to 3 years, at 4°C for up to 2 years, or in solution at -80°C for up to 6 months (or -20°C for up to 1 month) with protection from light. The TGF‑β signaling pathway plays critical roles in stemness maintenance, angiogenesis, fibrosis, and immune regulation . SRI-011381 has been used in studies investigating Alzheimer‘s disease, cancer stem cells, glioma stem cells, rotator cuff injury, embryo development, and neuroprotection . References include publications in Noncoding RNA Res (2025), SLAS Technol (2024), Dis Model Mech (2022), Molecular Cancer (2023), Experimental and Therapeutic Medicine (2021), and Nature Communications (2021) .
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| Molecular Formula |
C20H32CLN3O
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|---|---|
| Molecular Weight |
365.9406
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| Exact Mass |
365.223
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| Elemental Analysis |
C, 65.64; H, 8.81; Cl, 9.69; N, 11.48; O, 4.37
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| CAS # |
2070014-88-7
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| Related CAS # |
SRI-011381;1629138-41-5
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| PubChem CID |
122198132
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
369
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O=C(N([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])N(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])C1([H])C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H]
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| InChi Key |
GPNMJVSGNMDOJN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H31N3O.ClH/c24-20(22-19-9-5-2-6-10-19)23(15-17-7-3-1-4-8-17)16-18-11-13-21-14-12-18;/h1,3-4,7-8,18-19,21H,2,5-6,9-16H2,(H,22,24);1H
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| Chemical Name |
1-benzyl-3-cyclohexyl-1-(piperidin-4-ylmethyl)urea;hydrochloride
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| Synonyms |
SRI-011381 hydrochloride; SRI-011381 HCl; SRI011381 HCl; SRI-011381 (hydrochloride); 1-Benzyl-3-cyclohexyl-1-(piperidin-4-ylmethyl)urea hydrochloride; 1-benzyl-3-cyclohexyl-1-(piperidin-4-ylmethyl)urea;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) |
DMSO: 33.33 mg/mL (91.08 mM)
H2O: 25 mg/mL (68.32 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (136.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7327 mL | 13.6634 mL | 27.3269 mL | |
| 5 mM | 0.5465 mL | 2.7327 mL | 5.4654 mL | |
| 10 mM | 0.2733 mL | 1.3663 mL | 2.7327 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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