SUN B8155

• CAT Number: I010276
• CAS Number: 345893-91-6
• Molecular Formula: C14H15N3O3
• Molecular Weight: 273.29
• Purity: ≥95%
• Synonyms: 5-[N-(2-aminophenyl)-C-methylcarbonimidoyl]-1,6-dihydroxy-4-methylpyridin-2-one
• InChI: InChI=1S/C14H15N3O3/c1-8-7-12(18)17(20)14(19)13(8)9(2)16-11-6-4-3-5-10(11)15/h3-7,19-20H,15H2,1-2H3
• InChIKey: SGJLINMLDNLWOS-UHFFFAOYSA-N
• SMILES: CC1=CC(=O)N(C(=C1C(=NC2=CC=CC=C2N)C)O)O

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].
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].
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].

Reference

[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.
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