Molecular structure of Calhex 231, CAS Number: 652973-93-8
Calhex 231 (CAS 652973-93-8)
See product citations (16)
Application:
Calhex 231 is an inhibitor of the CaSR via negative allosteric modulation
CAS Number:
652973-93-8
Purity:
≥98%
Molecular Weight:
406.95
Molecular Formula:
C25H27ClN2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Calhex 231 is an inhibitor of the CaSR (calcium sensing receptor) via negative allosteric modulation. Calhex 231 blocks increases in [3H]inositol phosphate levels elicited by wild-type hCasR activation (IC50 = 0.39 μM in transiently transfected HEK293 cells).
Calhex 231 (CAS 652973-93-8) References
- Therapeutic approaches to bone diseases. | Rodan, GA. and Martin, TJ. 2000. Science. 289: 1508-14. PMID: 10968781
- Discoveries, drugs and skeletal disorders. | Goltzman, D. 2002. Nat Rev Drug Discov. 1: 784-96. PMID: 12360256
- Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca(2+)-sensing receptor. | Petrel, C., et al. 2003. J Biol Chem. 278: 49487-94. PMID: 14506236
- Positive and negative allosteric modulators of the Ca2+-sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain. | Petrel, C., et al. 2004. J Biol Chem. 279: 18990-7. PMID: 14976203
- The calcilytics Calhex-231 and NPS 2143 and the calcimimetic Calindol reduce vascular reactivity via inhibition of voltage-gated Ca2+ channels. | Greenberg, HZE., et al. 2016. Eur J Pharmacol. 791: 659-668. PMID: 27725162
- The Calcilytic Drug Calhex-231 Ameliorates Vascular Hyporesponsiveness in Traumatic Hemorrhagic Shock by Inhibiting Oxidative Stress and miR-208a-Mediated Mitochondrial Fission. | Lei, Y., et al. 2020. Oxid Med Cell Longev. 2020: 4132785. PMID: 33343806
- The calcimimetic R-568 attenuates subarachnoid hemorrhage-induced vasospasm through PI3K/Akt/eNOS signaling pathway in the rat model. | Güleç, İ., et al. 2021. Brain Res. 1765: 147508. PMID: 33930376
- SKF96365 activates calcium-sensing receptors in pulmonary arterial smooth muscle cells. | Miyaki, R., et al. 2022. Biochem Biophys Res Commun. 607: 44-48. PMID: 35366542
- Ca2+ Signaling and Proliferation via Ca2+-Sensing Receptors in Human Hepatic Stellate LX-2 Cells. | Kondo, R., et al. 2022. Biol Pharm Bull. 45: 664-667. PMID: 35491171
- Macrophages in obesity are characterised by increased IL-1β response to calcium-sensing receptor signals. | Thrum, S., et al. 2022. Int J Obes (Lond). 46: 1883-1891. PMID: 35931812
- Secretory Factors from Calcium-Sensing Receptor-Activated SW872 Pre-Adipocytes Induce Cellular Senescence and A Mitochondrial Fragmentation-Mediated Inflammatory Response in HepG2 Cells. | Briones-Suarez, L., et al. 2023. Int J Mol Sci. 24: PMID: 36982291
- Modulation of fibroblast growth factor-23 expression and transepithelial calcium absorption in Caco-2 monolayer by calcium-sensing receptor and calcineurin under calcium hyperabsorptive state. | Rodrat, M., et al. 2023. Biochem Biophys Res Commun. 659: 105-112. PMID: 37060830
- Stimulation of the calcium-sensing receptor induces relaxations of rat mesenteric arteries by endothelium-dependent and -independent pathways via BKCa and KATP channels. | Carlton-Carew, SRE., et al. 2024. Physiol Rep. 12: e15926. PMID: 38281732
Inhibitor of:
CaSR.Activator of:
CaSR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Calhex 231, 5 mg | sc-207394 | 5 mg | $347.00 |