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Submit ReviewR 568 hydrochloride
Description: Positive allosteric modulator of human calcium-sensing receptor (CaSR)
Chemical Name: 2-Chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanamine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for R 568 hydrochloride
R 568 hydrochloride is a positive allosteric modulator and allosteric agonist of the human calcium-sensing receptor (hCaSR). Exhibits calcimimetic activity. Has the ability to restore function to hCaSR mutants that cause familial hypocalciuric hypercalcemia (FHH) and neonatal severe hyperparathyroidism (NSHPT). Exerts a suppressive effect on parathyroid (PT) hormone secretion; inhibits PT cell proliferation in rats with renal insufficiency.
Compound Libraries for R 568 hydrochloride
R 568 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for R 568 hydrochloride
| M. Wt | 340.29 |
| Formula | C18H22ClNO.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 177172-49-5 |
| PubChem ID | 158796 |
| InChI Key | YJXUXANREVNZLH-PFEQFJNWSA-N |
| Smiles | ClC(C=CC=C2)=C2CCCN[C@H](C)C1=CC=CC(OC)=C1.Cl |
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.
Solubility Data for R 568 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.03 | 100 | |
| ethanol | 34.03 | 100 |
Preparing Stock Solutions for R 568 hydrochloride
The following data is based on the product molecular weight 340.29. 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 | 2.94 mL | 14.69 mL | 29.39 mL |
| 5 mM | 0.59 mL | 2.94 mL | 5.88 mL |
| 10 mM | 0.29 mL | 1.47 mL | 2.94 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
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Product Datasheets for R 568 hydrochloride
References for R 568 hydrochloride
References are publications that support the biological activity of the product.
Wada et al (1997) The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. J.Clin.Invest. 100 2977 PMID: 9399943
Fox et al (1999) NPS R-568: a type II calcimimetic compound that acts on parathyroid cell calcium receptor of rats to reduce plasma levels of parathyroid hormone and calcium. J.Pharmacol.Exp.Ther. 290 473 PMID: 10411552
Ying Lin Lu et al (2009) Effect of the calcimimetic R-568 [3-(2-chlorophenyl)-N-((1R)-1-(3-methoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor. J.Pharmacol.Exp.Ther. 331 775 PMID: 19759318
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Keywords: R 568 hydrochloride, R 568 hydrochloride supplier, R568, hydrochloride, HCl, allosteric, modulators, and, agonists, calcium-sensing, recptor, hCaSR, PAM, Calcium-Sensing, Receptor, 3815, Tocris Bioscience
14 Citations for R 568 hydrochloride
Citations are publications that use Tocris products. Selected citations for R 568 hydrochloride include:
Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376 PMID: 24327954
Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469 PMID: 22730443
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
Jiali et al (2020) Calcium-Sensing Receptors in Chondrocytes and Osteoblasts Are Required for Callus Maturation and Fracture Healing in Mice. J Bone Miner Res 35 143-154 PMID: 31498905
Yamamura et al (2015) Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension. Sci Transl Med 10 e0138384 PMID: 26375676
Yarova et al (2015) Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. EMBO Mol Med 7 284ra60 PMID: 25904744
Zhang et al (2019) Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine. Front Physiol 9 1922 PMID: 30697165
Sun et al (2018) Calcimimetic R568 reduced the blood pressure and improved aortic remodeling in spontaneously hypertensive rats by inhibiting local renin-angiotensin system activity. Exp Ther Med 16 4089 PMID: 30402152
Donald T et al (2021) Study of the Expression and Function of Calcium-Sensing Receptor in Human Skeletal Muscle. Int J Mol Sci 22 PMID: 34298895
Zhang et al (2017) Calcium-Sensing Receptor Stimulation in Cultured Glomerular Podocytes Induces TRPC6-Dependent Calcium Entry and RhoA Activation. Cell Physiol Biochem 43 1777 PMID: 29050010
Cheng (2012) Calcium-sensing receptor inhibits secretagogue-induced electrolyte secretion by intestine via the enteric nervous system. Am J Physiol Gastrointest Liver Physiol 303 G60 PMID: 22517767
Rodríguez-Hernández et al (2016) Cinacalcet inhibits neuroblastoma tumor growth and upregulates cancer-testis antigens. Oncotarget 7 16112 PMID: 26893368
Mathias et al (2019) Sensory Axon Growth Requires Spatiotemporal Integration of CaSR and TrkB Signaling. J Neurosci 39 5842-5860 PMID: 31123102
Tang et al (2018) Calcimimetic acts on enteric neuronal CaSR to reverse cholera toxin-induced intestinal electrolyte secretion. Sci Rep 8 7851 PMID: 29777154
Do you know of a great paper that uses R 568 hydrochloride from Tocris? Please let us know.
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