CYM 5520 |
رقم الكتالوجGC15765
One-Click Copy Product Info
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CYM 5520 هو ناهض انتقائي ومستقبل 1-فوسفات 2 (S1PR2) مع EC50 من 480 نانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1449747-00-5
Sample solution is provided at 25 µL, 10mM.
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CYM 5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480nM[1]. CYM 5520 is used in research on S1PR2-mediated bone metabolism/bone regeneration, tumor migration, inflammatory immune regulation, and receptor signaling pathways.
In vitro, CYM 5520 (10μM; 60min) significantly suppressed HGF-induced migration of HuH7 cells[2]. Treatment of HEK293T cells with CYM 5520 (10μM; 2h) induced a marked increase in phospho-ERK1/2 levels (a downstream marker of S1P2 activation)[3].
In vivo, CYM 5520 (10mg/kg; i.p.; 5 days/week; 6 weeks) corrected osteopenia and stimulated osteoblast activity in OVX C57Bl6J mice[4]. CYM 5520 (1mg/kg; i.p.; once daily; 28 days) increased the mRNA expression of osteoblast differentiation markers, including ALP, OPN, BSP, and osteocalcin, in the tibia of 8-week-old male mice[5].
References:
[1]. Satsu, Hideo, et al. "A sphingosine 1-phosphate receptor 2 selective allosteric agonist." Bioorganic & medicinal chemistry 21.17 (2013): 5373-5382.
[2]. Matsushima-Nishiwaki, Rie, et al. "Sphingosine 1-phosphate (S1P) reduces hepatocyte growth factor-induced migration of hepatocellular carcinoma cells via S1P receptor 2." PLoS One 13.12 (2018): e0209050.
[3]. Pitman, Melissa R., et al. "The sphingosine 1-phosphate receptor 2/4 antagonist JTE-013 elicits off-target effects on sphingolipid metabolism." Scientific reports 12.1 (2022): 454.
[4]. Weske, Sarah, et al. "Agonist-induced activation of the S1P receptor 2 constitutes a novel osteoanabolic therapy for the treatment of osteoporosis in mice." Bone 125 (2019): 1-7.
[5]. Matsuzaki, Etsuko, et al. "Sphingosine-1-phosphate receptor 2 agonist induces bone formation in rat apicoectomy and alveolar bone defect model." Journal of Dental Sciences 17.2 (2022): 787-794.
| Cell experiment [1]: | |
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Cell lines |
Human HCC-derived HuH7 cells. |
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Preparation Method |
The cultured cells were seeded (1×105 cells/well) onto the upper chamber in the serum-free RPMI-1640 medium. When indicated, the cells were pretreated with CYM 5520, in the upper chamber for 60min at 37°C. Then, HGF (30ng/ml) was added to the lower chamber for 23h at 37°C. The migrated cells adherent to the underside of the membrane were fixed with 4% paraformaldehyde and stained with 4’,6-diamidino-2-phenylindole (DAPI) solution. |
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Reaction Conditions |
10μM; 60min. |
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Applications |
CYM 5520 significantly suppressed the HGF-induced migration of HuH7 cells. |
| Animal experiment [2]: | |
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Animal models |
Mice |
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Preparation Method |
Mice were housed in SPF cages without any pathogens and with access to mouse chow and water ad libitum. Treatment was started 5 weeks after ovariectomy (OVX). CYM 5520 was administered intraperitoneally at 10mg/kg/day for 5 consecutive days per week for 6 weeks. |
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Dosage form |
10mg/kg; i.p.; 5 days/week; 6 weeks. |
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Applications |
CYM 5520 correct osteopenia and stimulate osteoblast activity in OVX mice. |
References: | |
| Cas No. | 1449747-00-5 | SDF | |
| Chemical Name | 1-[2-[2,5-dimethyl-1-(phenylmethyl)-1H-pyrrol-3-yl]-2-oxoethyl]-1,6-dihydro-6-oxo-3-pyridinecarbonitrile | ||
| Canonical SMILES | O=C1C=CC(C#N)=CN1CC(C2=C(C)N(CC3=CC=CC=C3)C(C)=C2)=O | ||
| Formula | C21H19N3O2 | M.Wt | 345.4 |
| الذوبان | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.8952 mL | 14.476 mL | 28.9519 mL |
| 5 mM | 579 μL | 2.8952 mL | 5.7904 mL |
| 10 mM | 289.5 μL | 1.4476 mL | 2.8952 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 24 reference(s) in Google Scholar.)