2. Signaling Pathways
  3. GPCR/G Protein
  4. CaSR
  5. CaSR Antagonist

CaSR Antagonist

CaSR Antagonists (14):

Cat. No. Product Name Effect Purity
  • HY-10007
    NPS-2143
    		Antagonist 99.94%
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.
  • HY-10171
    NPS-2143 hydrochloride
    		Antagonist 99.98%
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.
  • HY-N0546
    Ligustroflavone
    		Antagonist 99.74%
    Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
  • HY-50713
    Calcium-Sensing receptor antagonist I
    		Antagonist 98.95%
    Calcium-Sensing receptor antagonist I is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-14401
    Encaleret
    		Antagonist 99.88%
    Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 0.012 μM. Encaleret can promote the secretion of parathyroid hormone. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.
  • HY-15104
    Ronacaleret hydrochloride
    		Antagonist 99.81%
    Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret hydrochloride (SB 751689A) is used for the study of postmenopausal osteoporosis.
  • HY-15105
    SB-423562
    		Antagonist 99.66%
    SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 has the potential for osteoporosis research.
  • HY-15106
    SB-423557
    		Antagonist
    SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation.
  • HY-14752
    Ronacaleret
    		Antagonist
    Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis.
  • HY-103320
    Calhex 231
    		Antagonist
    Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM).
  • HY-153258
    CaSR antagonist-1
    		Antagonist
    CaSR antagonist-1 is a calcium sensing receptor (CaSR) antagonist with an IC50 value of 50 nM. CaSR antagonist-1 can be used for the research of disorders associated with abnormal bone or mineral homeostasis such as osteoporosis.
  • HY-N0546R
    Ligustroflavone (Standard)
    		Antagonist
    Ligustroflavone (Standard) is the analytical standard of Ligustroflavone (HY-N0546). This product is intended for research and analytical applications. Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
  • HY-15105A
    SB-423562 hydrochloride
    		Antagonist
    SB-423562 hydrochloride is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 hydrochloride has the potential for osteoporosis research.
  • HY-171446
    TAK-075
    		Antagonist
    TAK-075 is an orally active CaSR antagonist with an IC50 value of 0.94 nM. TAK-075 can stimulate the transient secretion of parathyroid hormone (PTH) in rats and can effectively prevent a significant reduction in PTH secretion caused by the accumulation of active metabolites, maintaining the normal secretion pattern of PTH. TAK-075 can be used in the research of metabolic diseases and osteoporosis.