Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
| Molecular Weight | 360.45 |
| Formula | C23H24N2O2 |
| CAS Number | 478963-79-0 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Anne M Roesler, et al. Calcium sensing receptor in developing human airway smooth muscle
[4] C Vahe, et al. Diseases associated with calcium-sensing receptor
| Related Calcium-sensing Receptor Products |
|---|
| Encaleret
Encaleret is an orally active calcium-sensitive receptor (CaSR) antagonist for studies related to osteoporosis and autosomal dominant hypocalcemia (ADH1). |
| SB-423562
SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 has the potential for osteoporosis research. |
| SB-423557
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation. |
| Etelcalcetide
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis. |
| Upacicalcet
Upacicalcet is a calcium-sensing receptor (CaSR) agonist being developed for the study of secondary hyperparathyroidism (SHPT). |
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