CaSR Antagonist

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.

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.

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.

Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC₅₀ of 12 nM. Encaleret exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.

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.

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.

SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 has the potential for osteoporosis research.

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.

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.

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).

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.

Encaleret (CLTX-305) sodium is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC₅₀ of 12 nM. Encaleret sodium exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret sodium can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.

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.

SB-423562 hydrochloride is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 hydrochloride has the potential for osteoporosis research.

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.

NPS-2143 (Standard) is the analytical standard of NPS-2143 (HY-10007). This product is intended for research and analytical applications. 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.