PTHR

Parathyroid hormone receptor

PTHR is a G protein-coupled receptor (GPCR) that regulates calcium and phosphate homeostasis, bone formation, and renal function. PTHR is activated by PTH, PTH-related peptide (PTHrP), and tuberoinfundibular peptide of 39 residues (TIP39), which activates G-protein and initiates downstream signaling cascades such as Gαs/cAMP/PKA signaling pathway. PTHR promotes the release of calcium ions from bones and increases the kidneys' reabsorption of calcium ions, thereby maintaining blood calcium homeostasis. PTHR also reduces blood phosphorus levels by promoting renal phosphorus excretion. PTHR participates in bone formation, cartilage development, and the development of the pancreas, teeth and mammary glands. PTHR exists in three isoforms, PTH1R, PTH2R and PTH3R. PTH1R has a high affinity for PTH and PTHrP and is the main receptor for calcium homeostasis regulation. PTH2R has a high affinity for TIP39 and is involved in the functional regulation of the central nervous system. PTH3R is mainly expressed in non-mammalian vertebrates and has a higher affinity for PTHrP. PTHR dysfunction could lead to Blomstrand’s lethal chondroplasia, Ollier’s disease, Jansen’s metaphyseal chondroplasia, hypoparathyroidism, hyperparathyroidism and osteoporosis^[1]^[2].

References:

[1]. Cheloha RW, et al., PTH receptor-1 signalling-mechanistic insights and therapeutic prospects. Nat Rev Endocrinol. 2015 Dec;11(12):712-24. [Content Brief]

[2]. On JS, et al., Evolution of parathyroid hormone receptor family and their ligands in vertebrate. Front Endocrinol (Lausanne). 2015 Mar 10;6:28. [Content Brief]

PTHR Isoform Specific Products:

PTHR Isoform Comparison

PTHR Related Products (34)
Antibodies (1)
PTHR Isoform Comparison

By Effects:	Inhibitor (1) Agonists (11) Ligand (1) Antagonists (6) Activators (5)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P4798

Osteostatin (1-5) amide (human, bovine, dog, horse, mouse, rabbit, rat)
Osteostatin (1-5) amide (human, bovine, dog, horse, mouse, rabbit, rat) (Human PTHrP (107-111) amide) is a C-terminal parathyroid hormone-related protein fragment that can inhibit bone resorption.

HY-P4701

pTH-Related Protein (1-34) amide (human, mouse, rat)
pTH-Related Protein (1-34) amide (human, mouse, rat) (Human PTHrP-(1-34)NH2) is a N-terminal fragments of PTHrP. pTH-Related Protein (1-34) amide (human, mouse, rat) induces hypercalcemia, and can be used for research of humoral hypercalcaemia of malignancy.

HY-186200

PTHR1 antagonist 1	Antagonist
PTHR1 antagonist 1 (Compound 18) is a PTHR1 antagonist with an IC₅₀ of 0.090 µM. PTHR1 antagonist 1 is applicable to the research of calcium metabolism disorders.

HY-P4684

Osteostatin
Osteostatin, a fragment of parathyroid hormone-related protein (PTHrP) 107-111, promotes bone repair in animal models of bone defects and prevents bone erosion in inflammatory arthritis, inhibits collagen-induced arthritis and inhibits osteoclastic bone resorption directly. Osteostatin can be used for inflammation and immunology research.

HY-P0059S

Teriparatide-d₁₀
Teriparatide-d₁₀ (Human parathyroid hormone-(1-34)-d₁₀) is the deuterium labeled Teriparatide (HY-P0059). Teriparatide (Human parathyroid hormone-(1-34)) is a PTH1 receptor agonist. Teriparatide (Human parathyroid hormone-(1-34)) can be used for osteoporosis research.

HY-131206

DS37571084	Antagonist
DS37571084 is an orally active and potent antagonist of the parathyroid hormone type 1 receptor (PTHR1), with an IC₅₀ value of 0.17 μM. DS37571084 can be used for the study of hyperparathyroidism.

HY-16498

Tigapotide	Inhibitor
Tigapotide (PCK-3145) is a synthetic 15-mer peptide derived from prostate-secretory protein, and acts as an antineoplastic agent. Tigapotide inhibits tumor growth, experimental bone metastasis, and malignancy-associated hypocalcemia. Tigapotide induces apoptosis in prostate cancer cells and tumors, and suppresses the growth of prostate cancer cells. Tigapotide inhibits the production of parathyroid hormone-related protein (PTHrP) in tumors and plasma. Tigapotide reduces plasma calcium levels in hypercalcemic tumor-bearing rats. Tigapotide is applicable for the research of prostate cancer and malignancy-associated hypercalcemia.

HY-120398

CH5447240	Agonist
CH5447240 is an agonist for parathyroid hormone receptor 1 (PTHR1), that inhibits human PTHR1 with an EC₅₀ of 12 μM. CH5447240 exhibits good metabolic stability in human liver microsomes. CH5447240 increases serum calcium levels in rats. CH5447240 can be used in research about hypoparathyroidism.

HY-32351B

3-epi-Calcifediol
3-epi-25-hydroxy Vitamin D3 is the C-3 epimer of 25-hydroxy vitamin D3.1 Dietary administration of 3-epi-25-hydroxy vitamin D3 (0.5 and 1 IU/g) decreases levels of serum parathyroid hormone (PTH) in male, but not female, weanling rats.

HY-179356

Octadecyl β-D-glucopyranosiduronic acid	Activator
Octadecyl β-D-glucopyranosiduronic acid (Compound 9) is a parathyroid hormone 1 receptor (PTH1R) activator, with a pEC₅₀ value > 9. Octadecyl β-D-glucopyranosiduronic acid can be used for research on hypoparathyroidism.

HY-32351BR

3-epi-Calcifediol (Standard)
3-epi-Calcifediol (Standard) is the analytical standard of 3-epi-Calcifediol. This product is intended for research and analytical applications. 3-epi-25-hydroxy Vitamin D3 is the C-3 epimer of 25-hydroxy vitamin D3.1 Dietary administration of 3-epi-25-hydroxy vitamin D3 (0.5 and 1 IU/g) decreases levels of serum parathyroid hormone (PTH) in male, but not female, weanling rats.

HY-100856R

PCO371 (Standard)	Agonist
PCO371 (Standard) is the analytical standard of PCO371 (HY-100856). This product is intended for research and analytical applications. PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.

HY-106288R

Human PTHrP-(1-36) (Standard)
Human PTHrP-(1-36) (Standard) is the analytical standard of Human PTHrP-(1-36) (HY-106288). This product is intended for research and analytical applications. Human PTHrP-(1-36) is a secretory form of PTHrP with anticalciuric effects. Human PTHrP-(1-36) enhances beta cell function and proliferation. Human PTHrP-(1-36) can be used in the research of humoral hypercalcemia of malignancy (HHM) and hyperparathyroidism.

HY-176946

PTH1R agonist 4	Agonist
PTH1R agonist 4 (Example 63) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC₅₀ value greater than 7. PTH1R agonist 4 can be used for the study of bone diseases, such as osteoporosis.

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PTHR

PTHR Isoform Specific Products:

PTHR Isoform Specific Products:

PTHR Related Products (34)

Antibodies (1)

PTHR Isoform Comparison

PTHR Related Products (34):