| Size | Price | Stock | Qty |
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| Targets |
PI3K/Akt[3]
YS-49 acts as an activator of PI3K/Akt signaling, which is a downstream target of RhoA. It reduces RhoA/PTEN activation in cells. YS-49 also activates cardiac beta-adrenoceptors, contributing to its strong positive inotropic effects. Additionally, it inhibits angiotensin II (Ang II)-stimulated proliferation of vascular smooth muscle cells (VSMCs) via the induction of heme oxygenase-1 (HO-1). It regulates Ang II-stimulated ROS production, JNK phosphorylation, and VSMC proliferation, reducing RhoA/PTEN activation. YS-49 is also a reported angiotensin receptor inhibitor. |
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| ln Vitro |
In both RAVSMC and RAW 264.7 cells exposed to lipopolysaccharide (LPS) plus INF-γ, YS-49 (1–100 μM; 18 hours) concentration-dependently reduces the buildup of nitrite, with IC50 values of 22 μM and 30 μM, respectively[2]. In RAVSMC and RAW 264.7 cells, YS-49 (10–100 μM; 18 hours) inhibits the transcriptional level of the iNOS gene expression that is triggered by LPS and/or cytokines[2].
In vitro, YS-49 (monohydrate) is a PI3K/Akt activator. It induces heme oxygenase-1 (HO-1) in endothelial cells and protects cells from oxidant injury. YS-49 inhibits Ang II-stimulated proliferation of vascular smooth muscle cells (VSMCs) through HO-1 production, which inhibits both the JNK pathway and ROS production. It concentration-dependently inhibits nitrite accumulation in RAVSMC and RAW 264.7 cells exposed to LPS plus INF-gamma, with IC50 values of 22 microM and 30 microM, respectively. YS-49 (10-100 microM; 18 hours) suppresses iNOS gene expression. The compound also activates cardiac beta-adrenoceptors, producing a strong positive inotropic effect, which is antagonized by a PI3K inhibitor (wortmannin). |
| ln Vivo |
Treatment with YS-49 (5 mg/kg; intraperitoneal injection; 8 hours; male Sprague Dawley rats) dramatically lowers blood NOx levels in animals treated with lipopolysaccharide (LPS); NOx levels drop from 86 μM to 34 μM[2].
In vivo, YS-49 (as CKD712, S-YS-49) confers cardiac protection and anti-inflammatory effects via activation of the PI3K signal pathway. These effects are antagonized by a PI3K inhibitor (wortmannin). The compound has been reported to protect cells from oxidant injury and reduce vascular smooth muscle cell proliferation. It has potential for the study of cardiovascular diseases, inflammation, and oxidative stress. |
| Enzyme Assay |
For in vitro PI3K/Akt activation assays, cells (e.g., endothelial cells or vascular smooth muscle cells) are serum-starved overnight, then treated with YS-49 at concentrations of 1-100 microM for 1-24 hours. Cell lysates are prepared, and Akt phosphorylation (p-Akt at Ser473 or Thr308) is measured by Western blot. Total Akt is used as a loading control. PI3K inhibitor (e.g., wortmannin 100 nM) can be used as a control to confirm pathway specificity. For iNOS expression assays, RAW 264.7 macrophages are treated with YS-49 (10-100 microM) for 1 hour, then stimulated with LPS (1 microg/mL) plus INF-gamma (10 ng/mL) for 18 hours. iNOS protein expression is measured by Western blot, and nitrite accumulation in the supernatant is measured by Griess assay. Cytotoxicity is assessed by MTT assay. For HO-1 induction assays, cells are treated with YS-49 (1-50 microM) for 6-24 hours. HO-1 protein expression is measured by Western blot.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: RAVSMC and RAW 264.7 cells Tested Concentrations: 10 μM, 30 μM and 100 μM(RAVSMC); 1 μM, 10 μM and 100 μM(RAW 264.7) Incubation Duration: 18 hrs (hours) Experimental Results: Inhibited the Accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to LPS+INF-γ, with IC50 values of 22 and 30 μM, respectively. Western Blot Analysis[2] Cell Types: RAVSMC and RAW 264.7 cells Tested Concentrations: 10 μM, 30 μM and 100 μM Incubation Duration: 18 hrs (hours) Experimental Results: Concentration-dependently inhibited the expression of iNOS protein induced by LPS plus IFN-γ. |
| Animal Protocol |
Animal/Disease Models: Male Sprague Dawley rats (250-300 g)[2]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip)injection; 8 hrs (hours) Experimental Results: Serum NOx levels were Dramatically decreased. For in vivo efficacy studies, YS-49 is dissolved in saline or formulated in a vehicle such as 10% DMSO in PBS. For cardiac protection studies, an animal model of myocardial ischemia-reperfusion injury or heart failure can be used. YS-49 is administered via intraperitoneal injection at doses of 1-10 mg/kg, either before ischemia or at the start of reperfusion. Cardiac function is assessed by echocardiography. Infarct size is measured by TTC staining. Biomarkers of oxidative stress and inflammation (e.g., MDA, SOD, TNF-alpha) are measured in cardiac tissue. For anti-inflammatory studies, an LPS-induced systemic inflammation model in mice can be used. YS-49 is administered intraperitoneally (1-10 mg/kg) 1 hour before LPS challenge (10 mg/kg). Blood and tissue samples are collected 4-6 hours post-LPS to measure serum cytokine levels (TNF-alpha, IL-1beta, IL-6) by ELISA and nitrite levels by Griess assay. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for YS-49 are limited. The molecular weight of YS-49 monohydrate is 420.32 (free base MW 317.38). The compound is soluble in water (>10 mg/mL) and DMSO. For in vitro studies, stock solutions can be prepared in DMSO and diluted in aqueous buffers. For in vivo studies, it can be administered via intraperitoneal or intravenous routes. YS-49 should be stored at 2-8degC as a solid. Specific PK parameters (half-life, Cmax, bioavailability) should be obtained from primary literature.
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| Toxicity/Toxicokinetics |
YS-49 monohydrate has been reported to protect cells from oxidant injury and is generally well tolerated in cell-based assays at concentrations up to 100 microM. In animal studies, it is safe at doses up to 10 mg/kg. The hazard classification includes Acute Toxicity Category 4 (oral). The compound has a warning label for acute oral toxicity. Standard safety precautions should be followed.
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| References |
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| Additional Infomation |
YS-49 monohydrate is a research-grade compound and is not approved for clinical use. It is an isoquinoline alkaloid analog of higenamine. YS-49 activates PI3K/Akt signaling and induces HO-1, providing cytoprotective and anti-inflammatory effects. It is used to study cardiovascular diseases, inflammation, oxidative stress, and PI3K/Akt signaling pathways. The CAS number is 3028631-24-2. The monohydrate form is a solid, soluble in water (>10 mg/mL). Store at 2-8degC.
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| Molecular Formula |
C20H22BRNO3
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|---|---|
| Molecular Weight |
404.3
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| Exact Mass |
403.078
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| CAS # |
3028631-24-2
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| Related CAS # |
YS-49;132836-42-1
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| PubChem CID |
71311929
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| Appearance |
Off-white to gray solid powder
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| Hydrogen Bond Donor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CNC(C2=CC(=C(C=C21)O)O)CC3=CC=CC4=CC=CC=C43.O.Br
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| InChi Key |
QHCUNMLYODPTIU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19NO2.BrH.H2O/c22-19-11-15-8-9-21-18(17(15)12-20(19)23)10-14-6-3-5-13-4-1-2-7-16(13)14;;/h1-7,11-12,18,21-23H,8-10H2;1H;1H2
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| Chemical Name |
1-(naphthalen-1-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol;hydrate;hydrobromide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4734 mL | 12.3671 mL | 24.7341 mL | |
| 5 mM | 0.4947 mL | 2.4734 mL | 4.9468 mL | |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4734 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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