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CaSR biased allosteric modulator (pEC50 = 7.8-8.1). Calcimimetic. Displays ability to bias signalling towards the accumulation of PERK1/2 and IP1. Reduces parathyroid hormone (PTH) levels in rat serum without inducing the release of calcitonin. Exhibits no significant activation of human GABAB or type I PTH receptors. Orally active.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 283.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.53 mL||17.64 mL||35.29 mL|
|5 mM||0.71 mL||3.53 mL||7.06 mL|
|10 mM||0.35 mL||1.76 mL||3.53 mL|
|50 mM||0.07 mL||0.35 mL||0.71 mL|
References are publications that support the biological activity of the product.
Cook et al (2015) Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics. Br.J.Pharmacol. 172 185 PMID: 25220431
Ma et al (2011) Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J.Pharmacol.Exp.Ther. 337 275 PMID: 21239511
Leach et al (2016) Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor. Cell.Res. 26 574 PMID: 27002221
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Keywords: AC 265347, AC 265347 supplier, AC265347, CaSR, biased, allosteric, modulator, calcimimetic, parathyroid, homrone, PTH, calcitonin, PERK1/2, IP1, accumulation, orally, active, Calcium-Sensing, Receptor, 6165, Tocris Bioscience
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