SR59230A |
Catalog No.GC39725
One-Click Copy Product Info
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SR59230A is a potent and selective β3-adrenoceptor antagonist, with IC50 values of 40, 408, and 648nM for β3-, β1-, and β2-receptors, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 174689-39-5
Sample solution is provided at 25 µL, 10mM.
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SR59230A is a potent and selective β3-adrenoceptor antagonist, with IC50 values of 40, 408, and 648nM for β3-, β1-, and β2-receptors, respectively [1]. SR59230A is a novel inhibitor of the Kir2.1 channel, with an IC50 value of 33μM[2]. SR59230A inhibits the phosphorylation and thereby the activation of the mTOR/p70S6K pathway, crosses the blood-brain barrier, and acts on β3 adrenoceptors[3-4]. SR59230A has been widely used to inhibit cancer cell progression and to develop novel combination therapies[5].
In vitro, SR59230A treatment for 72 hours significantly inhibited the proliferation of HUVEC, BRAF mutated 8505 C thyroid carcinoma cells, and U-87 cells with IC50 values of 6.45µM, 13.09µM, and 18.21µM, respectively[6]. Treatment with 10µM SR59230A for 48 hours induced apoptosis in K562, KCL22, HEL and HL60 cells under hypoxic conditions (1% O2)[7].
In vivo, SR59230A treatment via continuous intratumoral injection at a dose of 5mg/kg for 8 consecutive days led to a significant reduction in tumor volume and weight in the melanoma mouse model, and inhibited angiogenesis[8]. For a period of 5 weeks, 50µg of SR59230A (dissolved in DMSO) was injected into the tail vein every 3 days, which significantly inhibited the growth of breast cancer xenograft tumors in mice and reduced the expressions of p-mTOR S2448, p-4E-BP1 (T37/46), and p-mTOR S2481[9].
References:
[1] Kanzler S A, Januario A C, Paschoalini M A. Involvement of β3-adrenergic receptors in the control of food intake in rats[J]. Brazilian Journal of Medical and Biological Research, 2011, 44: 1141-1147.
[2] Kulzer M, Seyler C, Welke F, et al. Inhibition of cardiac Kir2. 1–2.3 channels by beta3 adrenoreceptor antagonist SR 59230A[J]. Biochemical and Biophysical Research Communications, 2012, 424(2): 315-320.
[3] Deng J, Jiang P, Yang T, et al. Targeting β3-adrenergic receptor signaling inhibits neuroblastoma cell growth via suppressing the mTOR pathway[J]. Biochemical and Biophysical Research Communications, 2019, 514(1): 295-300.
[4] Lob H E, Song J, Hurr C, et al. Deletion of p22phox-dependent oxidative stress in the hypothalamus protects against obesity by modulating β3-adrenergic mechanisms[J]. JCI insight, 2017, 2(2): e87094.
[5] Ascone M, Banella C, Amato R, et al. Abstract A048 SR59230A-induced ferroptosis sensitization of Ewing sarcoma cells via Beta-3 adrenergic receptor modulation: A novel therapeutic target[J]. Cancer Research, 2024, 84(17_Supplement): A048-A048.
[6] Bandini A, Biso L, Viaggi C, et al. Synergistic combination of the adrenergic antagonist SR59230A with common chemotherapeutic drugs and target therapies in cancer and endothelial cells[J]. Investigational New Drugs, 2025: 1-11.
[7] Calvani M, Dabraio A, Bruno G, et al. β3-adrenoreceptor blockade reduces hypoxic myeloid leukemic cells survival and Chemoresistance[J]. International Journal of Molecular Sciences, 2020, 21(12): 4210.
[8] Dal Monte M, Casini G, Filippi L, et al. Functional involvement of β3-adrenergic receptors in melanoma growth and vascularization[J]. Journal of molecular medicine, 2013, 91(12): 1407-1419.
[9] Zhou Z, Zhan J, Luo Q, et al. ADRB3 induces mobilization and inhibits differentiation of both breast cancer cells and myeloid-derived suppressor cells[J]. Cell Death & Disease, 2022, 13(2): 141.
| Cell experiment [1]: | |
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Cell lines |
Human umbilical vein endothelial cells (HUVECs) |
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Preparation Method |
HUVECs were cultured in MCDB131 medium supplemented with 10% heat-inactivated fetal bovine serum, 2mM L-glutamine, 10U/ml heparin, 10ng/ml epidermal growth factor (EGF), and 5ng/ml basic fibroblast growth factor, at 37 °C, 5% CO2, and 95% humidity. The cells (2×104) were seeded in 24-well sterile plastic plates and allowed to adhere overnight. The cells were treated with SR59230A (0.001, 0.1, 1, 10, and 100μM) for 72 hours, or treated with solvent as a control to assess cell viability. |
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Reaction Conditions |
0.001, 0.1, 1, 10, and 100μM; 72h |
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Applications |
SR59230A treatment inhibited the cell viability of HUVECs cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6J mice |
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Preparation Method |
Fifty male C57BL/6J mice (8 weeks old) were raised in a standard environment. The mice were injected with B16F10 cells and then received either SR59230A or L-748,337 treatment. SR59230A and L-748,337 were injected intratumorally at a dose of 5mg/kg/day. The treatment began on the 10th day (D10) after tumor cell injection and continued until D18. The length (L) and width (W) of the tumors were measured daily using a vernier caliper, and the tumor volume was calculated as the formula L×W2×0.5. |
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Dosage form |
5mg/kg/day for 9 days; intratumoral injection |
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Applications |
SR59230A treatment decreases the growth of melanoma in xenograft mouse model of B16F10 cells. |
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References: |
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| Cas No. | 174689-39-5 | SDF | |
| Canonical SMILES | O[C@@H](CN[C@H]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.O=C(O)C(O)=O | ||
| Formula | C23H29NO6 | M.Wt | 415.48 |
| Solubility | DMSO: 31.25 mg/mL (75.21 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4069 mL | 12.0343 mL | 24.0685 mL |
| 5 mM | 481.4 μL | 2.4069 mL | 4.8137 mL |
| 10 mM | 240.7 μL | 1.2034 mL | 2.4069 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)