Encaleret

Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1[1][2].

Product Specifications

CAS Number

[787583-71-5]

Product Name Alternative

CLTX-305; JTT-305; MK-5442

UNSPSC

12352005

Target

CaSR; Thyroid Hormone Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/encaleret.html

Concentration

10mM

Purity

99.88

Solubility

DMSO : 350 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C2=CC=CC=C2[C@H](OC[C@H](O)CNC(C)(C)CC3=CC=C(Cl)C(F)=C3)C)C=C1C)O

Molecular Formula

C29H33ClFNO4

Molecular Weight

514.03

References & Citations

[1]Gafni RI, et al. Efficacy and Safety of Encaleret in Autosomal Dominant Hypocalcemia Type 1. N Engl J Med. 2023 Sep 28;389 (13) :1245-1247.|[2]Shinagawa Y, et al. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone. ACS Med Chem Lett. 2010 Dec 29;2 (3) :238-42.