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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
CYM5520 (CYM-5520), a pyrrolyl ketone analog, is a novel, a potent, selective, and allosteric agonist of sphingosine-1-phosphate receptor 2 with anti-osteoporosis activity. It inhibits S1P2 with EC50 of 480 nM for S1PR2; Its binding is not competitive with JTE-013. CYM-5520 does not show any agonsit activity towards S1PR1, S1PR3, S1PR4 or S1PR5. It acts as a full agonist for both wild type and triple mutant S1PR2 (EC50 = 1.6 and 1.5 µM, respectively)
ln Vitro |
CYM-5520 is a complete agonist of wild-type S1PR2 with an EC50 of 1.6 μM. While CYM-5520 is an agonist with an EC50 of 1.5 μM, stimulating cells expressing the triple mutant S1PR2 with S1P does not stimulate luciferase activity [1].
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ln Vivo |
Following osteopenia resection surgery, CYM-5520 (10 mg/kg; intraperitoneal injection; 5 days per week; for 6 weeks) treatment significantly increased long bone and vertebral bone mass. In addition, CYM-5520 raises alkaline phosphatase, osteoblast counts, and the concentrated concentration of procollagen IC-terminal propeptide, a marker of bone anabolism [2].
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Animal Protocol |
Animal/Disease Models: Ovariectomized 12weeks old C57Bl6J mice[2]
Doses: 10 mg/kg Route of Administration: ip; 5 days per week; 6 weeks Experimental Results: Correction of ovariectomized mice by inducing new bone formation Osteopenia. |
References |
[1]. Hideo Satsu, et al. A sphingosine 1-phosphate receptor 2 selective allosteric agonist. Bioorg Med Chem. 2013 Sep 1;21(17):5373-82.
[2]. Sarah Weske, et al. Agonist-induced activation of the S1P receptor 2 constitutes a novel osteoanabolic therapy for the treatment of osteoporosis in mice. Bone. 2019 Aug;125:1-7. |
Molecular Formula |
C21H19N3O2
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Molecular Weight |
345.394464731216
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CAS # |
1449747-00-5
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SMILES |
N#CC(C=C1)=CN(CC(C2=C(C)N(CC3=CC=CC=C3)C(C)=C2)=O)C1=O
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InChi Key |
FMYGNANMYYHBSU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H19N3O2/c1-15-10-19(16(2)24(15)13-17-6-4-3-5-7-17)20(25)14-23-12-18(11-22)8-9-21(23)26/h3-10,12H,13-14H2,1-2H3
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Chemical Name |
1-[2-[2,5-Dimethyl-1-(phenylmethyl)-1H-pyrrol-3-yl]-2-oxoethyl]-1,6-dihydro-6-oxo-3-pyridinecarbonitrile
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Synonyms |
CYM-5520; CYM5520; CYM 5520.
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
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 : ~50 mg/mL (~144.76 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8953 mL | 14.4764 mL | 28.9528 mL | |
5 mM | 0.5791 mL | 2.8953 mL | 5.7906 mL | |
10 mM | 0.2895 mL | 1.4476 mL | 2.8953 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.