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CYM 5520

Names

[ CAS No. ]:
1449747-00-5

[ Name ]:
CYM 5520

[Synonym ]:
3-Pyridinecarbonitrile, 1-[2-[2,5-dimethyl-1-(phenylmethyl)-1H-pyrrol-3-yl]-2-oxoethyl]-1,6-dihydro-6-oxo-
MFCD28100815
1-[2-(1-Benzyl-2,5-dimethyl-1H-pyrrol-3-yl)-2-oxoethyl]-6-oxo-1,6-dihydro-3-pyridinecarbonitrile
CYM-5520

Biological Activity

[Description]:

CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> LPL Receptor
Research Areas >> Metabolic Disease

[In Vitro]

CYM-5520 (EC50 of 1.6 μM) is a full agonist for wild type S1PR2. Stimulation of cells expressing the triple mutant S1PR2 with S1P does not elicit a rise in luciferase activity, whereas the CYM-5520 is an agonist with an EC50 of 1.5 μM[1].

[In Vivo]

CYM-5520 (10 mg/kg; i.p.; 5 consecutive days per week; for 6 weeks) treatment clearly increases long bone and vertebral bone mass in osteopenic ovariectomized mice. CYM-5520 also increases osteoblast number, osteoid surface and alkaline phosphatase, and plasma concentrations of the osteoanabolic marker procollagen I C-terminal propeptide are also elevated[2]. Animal Model: Ovariectomized 12 weeks old C57Bl6J mice[2] Dosage: 10 mg/kg Administration: i.p.; 5 consecutive days per week; for 6 weeks Result: Corrected ovariectomy-induced osteopenia in mice by inducing new bone formation.

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
580.5±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H19N3O2

[ Molecular Weight ]:
345.395

[ Flash Point ]:
304.9±30.1 °C

[ Exact Mass ]:
345.147736

[ LogP ]:
2.52

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.611

[ Storage condition ]:
2-8°C

Safety Information

[ Symbol ]:

GHS05, GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H318

[ Precautionary Statements ]:
P280-P301 + P310-P305 + P351 + P338

[ Risk Phrases ]:
25-41

[ Safety Phrases ]:
26-39-45

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds