| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
SUN B8155 targets the calcitonin receptor. It is a non-peptide agonist that selectively mimics the biological effects of calcitonin. The calcitonin receptor is a G protein-coupled receptor (GPCR) that, when activated, stimulates cAMP formation through Gs protein coupling. Calcitonin receptors are primarily expressed in bone, kidney, and brain, and are involved in calcium homeostasis and bone metabolism. SUN B8155's non-peptide nature may offer advantages over peptide calcitonin, including oral bioavailability and improved stability.
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| 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].
In vitro, SUN B8155 induces cAMP formation in cells expressing recombinant human calcitonin receptors. This demonstrates its agonist activity at the calcitonin receptor through Gs protein coupling and adenylyl cyclase activation. Standard in vitro assays include cAMP accumulation assays in cells expressing human calcitonin receptors, receptor binding studies to confirm target engagement, and assessment of downstream signaling pathways. The compound's non-peptide nature makes it a valuable tool for studying calcitonin receptor pharmacology without the limitations of peptide-based compounds. |
| 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].
In vivo, SUN B8155 selectively mimics the biological effects of calcitonin. Calcitonin is involved in maintaining bone homeostasis, reducing bone resorption, and lowering serum calcium levels. SUN B8155 may produce similar effects in vivo, including reduction of osteoclast activity and bone resorption. The compound has been studied for potential applications in bone disorders such as osteoporosis, Paget's disease, and hypercalcemia. However, comprehensive in vivo efficacy data from published literature are limited. |
| Enzyme Assay |
For non-cell-based receptor binding assays, SUN B8155 can be evaluated using membrane preparations from cells expressing human calcitonin receptors. Radioligand binding displacement experiments are performed using a radiolabeled calcitonin receptor ligand (e.g., [125I]-calcitonin). Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 1-2 hours. Bound radioligand is separated from free by filtration through glass fiber filters. Nonspecific binding is determined in the presence of excess unlabeled calcitonin. IC50 or Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human calcitonin receptors (e.g., HEK293 or CHO cells) are cultured in appropriate media. For cAMP accumulation assays, cells are treated with various concentrations of SUN B8155 and cAMP levels are measured using ELISA or HTRF-based detection. Forskolin may be used as a positive control for cAMP stimulation. For signaling pathway assays, downstream markers such as PKA activation or CREB phosphorylation may be assessed. The compound's ability to induce cAMP formation confirms its agonist activity at the calcitonin receptor.
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| Animal Protocol |
For in vivo animal studies, SUN B8155 can be administered to rodents via oral or intraperitoneal administration. In bone metabolism models (e.g., ovariectomized rats for osteoporosis), bone mineral density, bone turnover markers (e.g., serum calcium, PTH, osteocalcin, CTX), and bone histomorphometry are assessed following compound administration. In models of hypercalcemia, serum calcium levels are measured. In models of Paget's disease, bone resorption markers are evaluated. Dosing regimens vary depending on the specific model.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of SUN B8155 have not been extensively characterized. As a non-peptide small molecule with a molecular weight of 273.29 and a molecular formula of C14H15N3O3, the compound is expected to have good oral bioavailability compared to peptide calcitonin. The compound has a purity of ≥97% by HPLC. Comprehensive ADME studies would be needed for full pharmacokinetic characterization, including assessment of oral bioavailability, half-life, protein binding, and tissue distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of SUN B8155 has not been extensively reported. As a calcitonin receptor agonist, potential adverse effects may include those associated with calcitonin, such as nausea, flushing, and injection site reactions (for peptide calcitonin). The non-peptide nature of SUN B8155 may reduce immunogenicity compared to peptide calcitonin. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on calcium homeostasis and bone metabolism.
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| References | |
| Additional Infomation |
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 peptide hormone that plays an important role in maintaining bone homeostasis. SUN B8155 induces cAMP formation in cells expressing recombinant human calcitonin receptors and has potential applications in bone disorders such as osteoporosis. As a non-peptide small molecule, it may offer advantages over peptide calcitonin, including oral bioavailability and reduced immunogenicity. The compound is available for research purposes only.
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| Molecular Formula |
C14H15N3O3
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|---|---|
| Molecular Weight |
273.29
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| Exact Mass |
273.111
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| CAS # |
345893-91-6
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| PubChem CID |
135484493
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.34g/cm3
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| Boiling Point |
419ºC at 760 mmHg
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| Flash Point |
207.2ºC
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| Index of Refraction |
1.637
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| LogP |
2.403
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=O)N(C(=C1C(=NC2=CC=CC=C2N)C)O)O
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| InChi Key |
SGJLINMLDNLWOS-UHFFFAOYSA-N
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| 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
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| Chemical Name |
5-[N-(2-aminophenyl)-C-methylcarbonimidoyl]-1,6-dihydroxy-4-methylpyridin-2-one
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (365.91 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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