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 |
|---|---|---|---|---|
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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. |
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V74615 | CaSR antagonist-1 | 1219811-83-2 | CaSR antagonist-1 is a calcium-sensing receptor (CaSR) antagonist (inhibitor) with IC50 of 50 nM. |
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V3463 | Cinacalcet (AMG-073) | 226256-56-0 | Cinacalcet (also known as AMG-073; trade names Sensipar, Mimpara) is a calcimimetic that mimics the action of calcium on tissues by allosteric activation of the calcium-sensing receptor expressed in various human organ tissues. |
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V1491 | Cinacalcet HCl (AMG-073) | 364782-34-3 | Cinacalcet HCl(also known as AMG-073; KRN1493; KRN-1493; Regpara; trade names Sensipar, Mimpara),the hydrochloride salt of Cinacalcet, is a calcimimetic that mimics the action of calcium on tissues by allosteric activation of the calcium-sensing receptor expressed in various human organ tissues. |
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V3932 | ETELCALCETIDE | 1262780-97-1 | Etelcalcetide (formerly known asAMG-416, KAI-4169; ONO5163; velcalcetide, trade name Parsabiv) is an FDA approved calcimimetic drug for the treatment of secondary hyperparathyroidism in chronic kidney disease (CKD) patients undergoing hemodialysis. |
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V3933 | ETELCALCETIDE HCL | 1334237-71-6 | Etelcalcetide HCl (formerly known as ONO-5163; AMG-416, KAI-4169 and velcalcetide, Parsabiv), the hydrochloride salt of Etelcalcetide, is an agonist of calcium-sensing receptor that has been approved by FDA in 2017 as a calcimimetic drug for the treatment of secondary hyperparathyroidism in CKD (chronic kidney disease) patients undergoing hemodialysis. |
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V74614 | Gadolinium chloride (Gadolinium(III) chloride; GdCl3) | 10138-52-0 | Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. |
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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. |
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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. |
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V74616 | SB-423562 | 351490-27-2 | SB-423562 is a short-acting (CaR) antagonist. |
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V0190 | Strontium Ranelate (S12911; Distrontium renelate) | 135459-87-9 | Strontium Ranelate (S-12911; Distrontium renelate; Protelos or Protos) is an approved antiosteoporotic drug in EU, it can also slow the course of osteoarthritis of the knee by both increasing bone formation and reducing bone resorption, leading to a rebalance of bone turnover in favor of bone formation. |
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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. |
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V74617 | Upacicalcet sodium | 2052969-18-1 | Upacicalcet sodium is an intravenous calcimimetic agent. |
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