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Encaleret

CAT: 0804-HY-14401-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14401-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3

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