The extracellular CaSR (calcium-sensing receptor) is a distinct G protein-coupled receptor (GPCR) that is activated by extracellular Ca2+ as well as by Mg2+, amino acids, and polyamines, among other physiological cations. The parathyroid gland, kidney, gut, and bone all express high levels of CaSR, which is the most crucial master controller of the extracellular Ca2+ homeostatic system. These tissues are where CaSR controls the release of parathyroid hormone (PTH), the production of vitamin D, and the absorption and resorption of Ca2+. Serious disruptions in extracellular Ca2+ metabolism are caused by gain and loss of function mutations in the CaSR.
Two significant signal transduction cascades are stimulated by the CaSR. The first is the production of inositol 1,4,5-trisphosphate (IP3) by Gq/11-phospholipase C (PLC), which causes a sharp increase in intracellular calcium (Ca2+i) concentrations. The second is the mitogen-activated protein kinases (MAPKs), which phosphorylate proteins mediating cytosolic signaling and translocate into the nucleus to activate transcription factors involved in cellular proliferation and differentiation. Examples of MAPKs include extracellular signal-regulated kinases 1 and 2 (ERK1/2). The G proteins Gq/11 and Gi/o, which prevent the synthesis of cyclic adenosine monophosphate (cAMP), as well as a potential G protein-independent mechanism involving -arrestin types 1 and 2, have been shown to be necessary for the CaSR's activation of MAPK signaling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V119374 | AXT-914 | 717104-43-3 | AXT-914 is a calcium-sensitive receptor (CaSR) inhibitor. |
|
V83422 | Calhex 231 | 652973-93-8 | |
|
V74618 | Calindol hydrochloride | 729610-18-8 | Calindol HCl is a positive allosteric modulator (PAM) of the calcimimetic calcium-sensing receptor (CaSR) with EC50 of 132 nM. |
|
V74615 | CaSR antagonist-1 | 1219811-83-2 | CaSR antagonist-1 is a calcium-sensing receptor (CaSR) antagonist (inhibitor) with IC50 of 50 nM. |
|
V110408 | Encaleret sodium | 787584-62-7 | Encaret sodium (CLTX-305) is an orally effective calcium-sensitive receptor (CaSR) antagonist with an IC50 value of 12 nM. |
|
V74614 | Gadolinium chloride (Gadolinium(III) chloride; GdCl3) | 10138-52-0 | Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. |
|
V106348 | Gamma-Glu-Abu TFA | Gamma-Glu-Abu TFA is the TFA salt form of Gamma-Glu-Abu. | |
|
V136846 | Gosicalcetide | 2650595-42-7 | Gosicalcetide is a calcium-sensitive receptor (CaSR) agonist. |
|
V107802 | H-Glu-Thr-OH | 6875-80-5 | H-Glu-Thr-OH (L-α-glutamyl-L-threonine) is a dipeptide composed of two amino acids, glutamate (Glu) and threonine (Thr), connected by a peptide bond and is an extracellular calcium-sensing receptor (CaSR) agonist. |
|
V112116 | KP-2067 | 1262781-19-0 | KP-2067 is a CaSR receptor agonist peptide. |
|
V98042 | NBI-35965 | 268546-19-6 | NBI-35965 is an antagonist of corticotropin-releasing factor receptor 1 (CRF-R1). |
|
V1492 | NPS-2143 (SB-262470) | 284035-33-2 | NPS-2143 (also called SB262470; NPS-2143; SB-262470; NPS 2143; SB-262470A) is a potent and selective antagonist of calcium-sensing receptor (CaSR) with the potential to be used for the treatment of osteoporosis. |
|
V30916 | NPS-2143 hydrochloride (SB-262470A) | 324523-20-8 | NPS-2143 HCl (also known as SB-262470 and SB-262470A) is a novel, potent and selective antagonist of calcium-sensing receptor (CaSR) with IC50 of 43 nM. |
|
V141613 | NPS-467 | 148717-47-9 | NPS-467 is a calcium receptor (CaR) activator and a stereoselective drug, with only its R-enantiomer being active. |
|
V83453 | Ronacaleret (SB 751689) | 753449-67-1 | |
|
V74616 | SB-423562 | 351490-27-2 | SB-423562 is a short-acting (CaR) antagonist. |
|
V145544 | TAK-075 | 667931-33-1 | TAK-075 is an orally effective calcium-sensitive receptor (CaSR) antagonist with an IC50 value of 0.94 nM. |
|
V94638 | Tecalcet | 148717-54-8 | Tecalcet (R 568) is an oral calcimimetic that allosterically positively regulates the calcium-sensing receptor (CaSR). |
|
V13565 | Tecalcet HCl (KRN568; NPS-R568; R568) | 177172-49-5 | Tecalcet (KRN-568; NPS-R-568; R-568) is a novel, potent, orally bioactive calcimimetic compound/calcium channel agonist that can be potentially used for the treatment of hyperparathyroidism, postmenopausal symptom. |
|
V74617 | Upacicalcet sodium | 2052969-18-1 | Upacicalcet sodium is an intravenous calcimimetic agent. |
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