Date published: 2025-10-2

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CaSR Activators

Calcium-Sensing Receptor (CaSR) activators are a unique class of compounds primarily characterized as calcimimetics. These activators play a crucial role in modulating the function of the CaSR, a G protein-coupled receptor (GPCR) that is vital in maintaining calcium homeostasis in the human body. The CaSR is predominantly expressed in the parathyroid glands and the kidneys, where it senses changes in extracellular calcium concentrations and accordingly regulates parathyroid hormone secretion and renal calcium reabsorption. The primary mechanism of action of CaSR activators involves allosteric modulation of the receptor. Compounds like Cinacalcet, NPS R-568, and Evocalcet bind to the allosteric sites on the CaSR, distinct from the orthosteric calcium-binding site. This binding enhances the receptor's sensitivity to extracellular calcium, leading to its activation even at lower calcium levels. Such activation typically results in the inhibition of parathyroid hormone secretion, thereby reducing serum calcium levels. The chemical diversity within this group ranges from small molecules to peptide-based compounds. Small molecules like Calhex 231 and GSK3004774 offer the advantage of oral bioavailability and selective receptor targeting. On the other hand, peptide-based activators like AMG 416 (Etalcalcetide) provide high specificity and potency in receptor activation. The development of newer compounds such as JTT-305/MK-5442 continues to expand the pharmacological landscape of CaSR activators. Their development underscores a significant trend in drug discovery, focusing on the precise modulation of receptor activity to achieve desired outcomes. Overall, CaSR activators represent a critical advancement in our understanding and ability to modulate GPCR function, particularly in calcium homeostasis and related disorders.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Cinacalcet Hydrochloride

364782-34-3sc-207438
10 mg
$230.00
7
(1)

Cinacalcet Hydrochloride acts as a potent allosteric modulator of the calcium-sensing receptor (CaSR), influencing its conformational dynamics. By stabilizing the active state of CaSR, it enhances the receptor's sensitivity to extracellular calcium levels. This modulation alters downstream signaling pathways, particularly those involving parathyroid hormone secretion and calcium homeostasis. Its unique interaction profile allows for nuanced regulation of cellular responses to calcium fluctuations.

R 568 hydrochloride

177172-49-5sc-361302
sc-361302A
10 mg
50 mg
$210.00
$860.00
4
(1)

R 568 hydrochloride serves as a selective allosteric enhancer of the calcium-sensing receptor (CaSR), promoting its activation through distinct molecular interactions. This compound exhibits a unique binding affinity that fine-tunes the receptor's response to calcium ions, thereby influencing intracellular signaling cascades. Its kinetic properties facilitate rapid receptor activation, leading to enhanced modulation of calcium-related pathways, which underscores its role in cellular calcium regulation.

AC-265347

1253901-26-6sc-364395
sc-364395A
5 mg
25 mg
$87.00
$370.00
1
(0)

AC-265347 functions as a potent modulator of the calcium-sensing receptor (CaSR), exhibiting a unique mechanism of action through specific allosteric binding sites. This compound engages in distinctive molecular interactions that stabilize the receptor's active conformation, thereby amplifying its sensitivity to extracellular calcium levels. The compound's dynamic kinetics enable swift receptor activation, influencing downstream signaling pathways and contributing to the intricate regulation of calcium homeostasis within cells.

Strontium chloride

10476-85-4sc-258180
5 g
$100.00
(0)

Strontium chloride acts as a selective modulator of the calcium-sensing receptor (CaSR), characterized by its ability to mimic calcium ions in binding affinity. This compound facilitates unique ionic interactions that enhance receptor activation, promoting a conformational shift that influences intracellular signaling cascades. Its distinct solubility properties allow for effective diffusion in biological systems, impacting the receptor's responsiveness to fluctuating calcium concentrations and modulating cellular calcium dynamics.

Calindol hydrochloride

729610-18-8sc-211006
10 mg
$400.00
8
(1)

Calindol is a calcimimetic agent that acts on the CaSR, enhancing its response to extracellular calcium ions and activating the receptor.

Calhex 231

652973-93-8sc-207394
5 mg
$340.00
16
(1)

Calhex 231 is a non-peptide calcimimetic agent that selectively activates CaSR, enhancing its response to extracellular calcium.