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CaSR

CaSR

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.

CaSR related products

Structure Cat No. Product Name CAS No. Product Description
Calhex 231 V83422 Calhex 231 652973-93-8
Calindol hydrochloride 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.
CaSR antagonist-1 V74615 CaSR antagonist-1 1219811-83-2 CaSR antagonist-1 is a calcium-sensing receptor (CaSR) antagonist (inhibitor) with IC50 of 50 nM.
Gadolinium chloride (Gadolinium(III) chloride; GdCl3) V74614 Gadolinium chloride (Gadolinium(III) chloride; GdCl3) 10138-52-0 Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist.
NBI-35965 V98042 NBI-35965 268546-19-6 NBI-35965 is an antagonist of corticotropin-releasing factor receptor 1 (CRF-R1).
NPS-2143 (SB-262470) 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.
NPS-2143 hydrochloride (SB-262470A) 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.
Ronacaleret (SB 751689) V83453 Ronacaleret (SB 751689) 753449-67-1
SB-423562 V74616 SB-423562 351490-27-2 SB-423562 is a short-acting (CaR) antagonist.
Tecalcet V94638 Tecalcet 148717-54-8 Tecalcet (R 568) is an oral calcimimetic that allosterically positively regulates the calcium-sensing receptor (CaSR).
Tecalcet HCl (KRN568; NPS-R568; R568) 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.
Upacicalcet sodium V74617 Upacicalcet sodium 2052969-18-1 Upacicalcet sodium is an intravenous calcimimetic agent.
Z8554052021 V84830 Z8554052021
依特卡肽 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.
盐酸乙酯 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.
盐酸西那卡塞 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.
西那卡塞 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.
雷奈酸锶 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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