CYM 5520

Names

[ 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

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.