PeptideDB

SUN B8155 345893-91-6

SUN B8155 345893-91-6

CAS No.: 345893-91-6

SUN B8155 is a non-peptide agonist of the calcitonin receptor that selectively mimics the biological effects of calciton
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This product is for research use only, not for human use. We do not sell to patients.

SUN B8155 is a non-peptide agonist of the calcitonin receptor that selectively mimics the biological effects of calcitonin. Calcitonin is a 32-amino acid (AA) peptide hormone secreted primarily by the thyroid gland and plays an important role in maintaining bone homeostasis.

Physicochemical Properties


Molecular Formula C14H15N3O3
Molecular Weight 273.29
Exact Mass 273.111
CAS # 345893-91-6
PubChem CID 135484493
Appearance Light yellow to yellow solid powder
Density 1.34g/cm3
Boiling Point 419ºC at 760 mmHg
Flash Point 207.2ºC
Index of Refraction 1.637
LogP 2.403
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 2
Heavy Atom Count 20
Complexity 508
Defined Atom Stereocenter Count 0
InChi Key SGJLINMLDNLWOS-UHFFFAOYSA-N
InChi Code

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
Chemical Name

5-[N-(2-aminophenyl)-C-methylcarbonimidoyl]-1,6-dihydroxy-4-methylpyridin-2-one
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro In T47D cells, SUN B8155 (1-1000 μM; 1 hour) increases intracellular cAMP production in a concentration-dependent manner; at the highest dose, the concentration of produced cAMP increased by about 42-fold. Additionally, SUN B8155 promotes the production of cAMP in the rat osteogenic sarcoma-derived cell line UMR106-06[1]. While SUN B8155 completely promotes cAMP formation in CHO/hCTR cells in a concentration-dependent manner with an EC50 of 21 μM, it does not stimulate cAMP formation in CHO/hPTHR or parental CHO cells[1].
ln Vivo Thirty minutes after delivery, SUN B8155 (100 mg/kg; ip) significantly lowers the serum calcium content by about 9%. Serum calcium levels are also lowered by human CT in a dose-dependent manner at 30 and 60 minutes (0.1 and 0.3 μg/kg) following administration[1].
References

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


Solubility Data


Solubility (In Vitro) DMSO: 100 mg/mL (365.91 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6591 mL 18.2956 mL 36.5912 mL
5 mM 0.7318 mL 3.6591 mL 7.3182 mL
10 mM 0.3659 mL 1.8296 mL 3.6591 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.