Calcium-Sensing Receptor Antagonists ICaSR antagonist CAS# 478963-79-0 |
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Quality Control & MSDS
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| Cas No. | 478963-79-0 | SDF | Download SDF |
| PubChem ID | 10109178 | Appearance | Powder |
| Formula | C23H24N2O2 | M.Wt | 360.46 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (277.43 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-propan-2-yl-4-(4-propan-2-ylphenyl)-6-prop-2-ynoxyquinazolin-2-one | ||
| SMILES | CC(C)C1=CC=C(C=C1)C2=NC(=O)N(C3=C2C=C(C=C3)OCC#C)C(C)C | ||
| Standard InChIKey | RXVZJHDMMKTKDR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H24N2O2/c1-6-13-27-19-11-12-21-20(14-19)22(24-23(26)25(21)16(4)5)18-9-7-17(8-10-18)15(2)3/h1,7-12,14-16H,13H2,2-5H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
IC50 value:
Target: CaSR
Calcium-Sensing Receptor Antagonists I is useful for osteoporosis and other bone conditions References: | |||||
Calcium-Sensing Receptor Antagonists I Dilution Calculator
Calcium-Sensing Receptor Antagonists I Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7742 mL | 13.8712 mL | 27.7423 mL | 55.4847 mL | 69.3558 mL |
| 5 mM | 0.5548 mL | 2.7742 mL | 5.5485 mL | 11.0969 mL | 13.8712 mL |
| 10 mM | 0.2774 mL | 1.3871 mL | 2.7742 mL | 5.5485 mL | 6.9356 mL |
| 50 mM | 0.0555 mL | 0.2774 mL | 0.5548 mL | 1.1097 mL | 1.3871 mL |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.5548 mL | 0.6936 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Calcium-Sensing Receptor Antagonists I is antagonists of calcium-sensing parathyroid hormone receptors.
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Novel and potent calcium-sensing receptor antagonists: discovery of (5R)-N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahy dropyrazolo[1,5-a]pyrimidine-3-carboxamide monotosylate (TAK-075) as an orally active bone anabolic agent.[Pubmed:21353570]
Bioorg Med Chem. 2011 Mar 15;19(6):1881-94.
The calcium-sensing receptor antagonist (CaSR) has been recognized as a promising target of anabolic agents for treating osteoporosis. In the course of developing a new drug candidate for osteoporosis, we found tetrahydropyrazolopyrimidine derivative 1 to be an orally active CaSR antagonist that stimulated transient PTH secretion in rats. However, compound 1 showed poor physical and chemical stability. In order to work out this compound's chemical stability and further understand its in vivo efficacy, we focused on modifying the 2-position of the tetrahydropyrazolopyrimidine. As a result of chemical modification, we discovered (5R)-N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahy dropyrazolo[1,5-a]pyrimidine-3-carboxamide monotosylate 10m (TAK-075), which showed improved solubility, chemical stability, and in vivo efficacy. Furthermore, we describe that evaluating the active metabolite is important during repeated treatment with short-acting CaSR antagonists.
Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.[Pubmed:27397499]
Bioorg Med Chem Lett. 2016 Aug 15;26(16):4077-80.
In a search for novel small molecule calcium-sensing receptor (CaSR) antagonists as oral bone anabolic agents, we discovered dihydrobenzofuran cyclopropane carboxylic acid derivatives, such as 12f (IC50=27.6nM), are highly potent calcium-sensing receptor antagonists. Studies in rats established that compound 12f stimulates parathyroid hormone (PTH) release in a fast-acting, pulsatile manner.
Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma.[Pubmed:25904744]
Sci Transl Med. 2015 Apr 22;7(284):284ra60.
Airway hyperresponsiveness and inflammation are fundamental hallmarks of allergic asthma that are accompanied by increases in certain polycations, such as eosinophil cationic protein. Levels of these cations in body fluids correlate with asthma severity. We show that polycations and elevated extracellular calcium activate the human recombinant and native calcium-sensing receptor (CaSR), leading to intracellular calcium mobilization, cyclic adenosine monophosphate breakdown, and p38 mitogen-activated protein kinase phosphorylation in airway smooth muscle (ASM) cells. These effects can be prevented by CaSR antagonists, termed calcilytics. Moreover, asthmatic patients and allergen-sensitized mice expressed more CaSR in ASMs than did their healthy counterparts. Indeed, polycations induced hyperreactivity in mouse bronchi, and this effect was prevented by calcilytics and absent in mice with CaSR ablation from ASM. Calcilytics also reduced airway hyperresponsiveness and inflammation in allergen-sensitized mice in vivo. These data show that a functional CaSR is up-regulated in asthmatic ASM and targeted by locally produced polycations to induce hyperresponsiveness and inflammation. Thus, calcilytics may represent effective asthma therapeutics.
Calcilytics: antagonists of the calcium-sensing receptor for the treatment of osteoporosis.[Pubmed:21526895]
Future Med Chem. 2011 Apr;3(5):535-47.
The only bone anabolic agents currently available on the market are based on the parathyroid hormone (PTH). Secretion of endogenous PTH is controlled by a calcium-sensing receptor at the surface of the parathyroid glands. Antagonists of this receptor (calcilytics) induce the release of the hormone. Provided the effect of the calcilytic is of short duration, a bone anabolic effect should also result. Although the first calcilytic series became known approximately 10 years ago, the number of different structural types is still small today. This article outlines the quest from hits to potent development candidates of all relevant calcilytic series currently known. Even after the front-runners unexpectedly failed in the clinic, the approach for an oral alternative to parenteral PTH remains highly attractive.
