R 568 hydrochloride

Catalog #: 3815
14 Citations Datasheet / COA / SDS

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R 568 hydrochloride | CAS No. 177172-49-5 | Calcium-Sensing Receptor Modulators

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Description: Positive allosteric modulator of human calcium-sensing receptor (CaSR)

Chemical Name: 2-Chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanamine hydrochloride

Purity: ≥99%

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Product Details

Citations (14)

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Biological Activity

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.

Technical Data

M.Wt:

340.29

Formula:

C₁₈H₂₂ClNO.HCl

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

≥99%

Storage:

Desiccate at RT

CAS No:

177172-49-5

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.

Background References

The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
Nature, 2012;492(7427):123-7.
K+ efflux agonists induce NLRP3 inflammasome activation independently of Ca2+ signaling.
Katsnelson M, Rucker L, Russo H, Dubyak G
J Immunol, 2015;194(8):3937-52.
The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency.
Wada et al.
J.Clin.Invest., 1997;100:2977
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.
Fox et al.
J.Pharmacol.Exp.Ther., 1999;290:473
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.
Ying Lin Lu et al.
J.Pharmacol.Exp.Ther., 2009;331:775

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for R 568 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for R 568 hydrochloride include:

14 Citations: Showing 1 - 10

Study of the Expression and Function of Calcium-Sensing Receptor in Human Skeletal Muscle.
Authors: Donald T Et al.
Int J Mol Sci 2021;22
Calcium-Sensing Receptors in Chondrocytes and Osteoblasts Are Required for Callus Maturation and Fracture Healing in Mice.
Authors: Jiali Et al.
J Bone Miner Res 2020;35:143-154
Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine.
Authors: Zhang Et al.
Front Physiol 2019;9:1922
Sensory Axon Growth Requires Spatiotemporal Integration of CaSR and TrkB Signaling.
Authors: Mathias Et al.
J Neurosci 2019;39:5842-5860
Calcimimetic acts on enteric neuronal CaSR to reverse cholera toxin-induced intestinal electrolyte secretion.
Authors: Tang Et al.
Sci Rep 2018;8:7851
Calcimimetic R568 reduced the blood pressure and improved aortic remodeling in spontaneously hypertensive rats by inhibiting local renin-angiotensin system activity.
Authors: Sun Et al.
Exp Ther Med 2018;16:4089
Calcium-Sensing Receptor Stimulation in Cultured Glomerular Podocytes Induces TRPC6-Dependent Calcium Entry and RhoA Activation.
Authors: Zhang Et al.
Cell Physiol Biochem 2017;43:1777
Cinacalcet inhibits neuroblastoma tumor growth and upregulates cancer-testis antigens.
Authors: Rodríguez-Hernández Et al.
Oncotarget 2016;7:16112
Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.
Authors: Yarova Et al.
EMBO Mol Med 2015;7:284ra60
Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension.
Authors: Yamamura Et al.
Sci Transl Med 2015;10:e0138384

Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
Authors: Engelstoft Et al.
Mol Metab 2013;2:376

The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca²⁺ and cAMP.
Authors: Lee Et al.
Nature 2012;492:123

Calcium-sensing receptor inhibits secretagogue-induced electrolyte secretion by intestine via the enteric nervous system.
Authors: Cheng
Am J Physiol Gastrointest Liver Physiol 2012;303:G60

Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension.
Authors: Yamamura Et al.
Circ Res 2012;111:469

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