SUN B8155

Names

[ Name ]:
SUN B8155

[Synonym ]:
5-[1-[(2-Aminophenyl)imino]ethyl]-1,6-dihydroxy-4-methyl-2(1H)-pyridinone

Biological Activity

[Description]:

SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CGRP Receptor

Research Areas >> Endocrinology

Signaling Pathways >> Neuronal Signaling >> CGRP Receptor

[In Vitro]

SUN B8155 (1-1000 μM; 1 hour) stimulates intracellular cAMP formation in T47D cells in a concentration-dependent manner; the concentration of synthesized cAMP increased by approximately 42-fold at the highest concentration. SUN B8155 also stimulates cAMP formation in the rat osteogenic sarcoma-derived cell line, UMR106-06[1]. SUN B8155 does not stimulate cAMP formation in CHO/hPTHR or parental CHO cells, but fully stimulates cAMP formation in CHO/hCTR cells in a concentration-dependent manner with an EC50 of 21 μM[1].

[In Vivo]

SUN B8155 (100 mg/kg; i.p.) results in a significant reduction of serum calcium concentration by approximately 9% at 30 min after administration. Human CT also reduces serum calcium in a dose-dependent manner at 30 min (0.1 and 0.3 μg/kg) and 60 min (0.3 μg/kg) after administration[1].

[References]

[1]. Katayama T, et al. Discovery of a non-peptide small molecule that selectively mimics the biological actions of calcitonin. Biochim Biophys Acta. 2001;1526(2):183-190.

Chemical & Physical Properties

[ Density]:
1.34g/cm3

[ Boiling Point ]:
419ºC at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₅N₃O₃

[ Molecular Weight ]:
273.28700

[ Flash Point ]:
207.2ºC

[ Exact Mass ]:
273.11100

[ PSA ]:
100.84000

[ LogP ]:
2.40370

[ Index of Refraction ]:
1.637

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ RIDADR ]:
UN 2811 6.1 / PGIII

Articles

Discovery of a non-peptide small molecule that selectively mimics the biological actions of calcitonin.

Biochim. Biophys. Acta 1526 , 183-190, (2001)

Calcitonin (CT), a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis. To discover non-peptide small molecules with biologica...