Molecular structure of SB 218795, CAS Number: 174635-53-1
SB 218795 (CAS 174635-53-1)
Application:
SB 218795 is a potent and selective NK3 antagonist
CAS Number:
174635-53-1
Purity:
≥98%
Molecular Weight:
396.44
Molecular Formula:
C25H20N2O3
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
SB 218795 belongs to the class of 2-phenyl-4-quinolinecarboxamides and acts as a specific, reversible, non-peptide, and competitive antagonist of the human NK-3 receptor. It hinders NK-3 receptor-mediated miosis. The characteristics of SB 218795 make it suitable for investigating the functional roles of NK-3 receptors. SB 218795 demonstrates robust selectivity as an antagonist of the NK3 receptor, exhibiting a Ki value of 13 nM for the human NK3 receptor, with approximately 90-fold and 7000-fold preference for the human NK3 receptor over the human NK2 and NK1 receptors, respectively.
SB 218795 (CAS 174635-53-1) References
- Transcripts of neurokinin B and neurokinin 3 receptor in superovulated rat ovaries and increased number of corpora lutea as a non-specific effect of intraperitoneal agonist application. | Löffler, S., et al. 2004. Regul Pept. 122: 131-7. PMID: 15380930
- Postsynaptic actions of substance P on rat periaqueductal grey neurons in vitro. | Drew, GM., et al. 2005. Neuropharmacology. 49: 587-95. PMID: 15921708
- Involvement of Ca2+ signaling in tachykinin-mediated contractile responses in swine trachea. | Lin, YR., et al. 2005. J Biomed Sci. 12: 547-58. PMID: 15971006
- Synthesis of new 4-heteroaryl-2-phenylquinolines and their pharmacological activity as NK-2/NK-3 receptor ligands. | Borioni, A., et al. 2007. Arch Pharm (Weinheim). 340: 17-25. PMID: 17206605
- Neurokinin-3 peptide instead of neurokinin-1 synergistically exacerbates kainic acid-inducing degeneration of neurons in the substantia nigra of mice. | Chen, LW., et al. 2008. J Neurochem. 105: 203-16. PMID: 18021294
- Rat urinary bladder-derived relaxant factor: studies on its nature and release by coaxial bioassay system. | Bozkurt, TE. and Sahin-Erdemli, I. 2008. Eur J Pharmacol. 591: 273-9. PMID: 18621043
- A1 and A2a receptors mediate inhibitory effects of adenosine on the motor activity of human colon. | Fornai, M., et al. 2009. Neurogastroenterol Motil. 21: 451-66. PMID: 19019012
- The investigation into indomethacin-induced potentiation of the contractile response to antigen in ovalbumin-sensitized guinea-pig tracheas. | Bozkurt, TE., et al. 2012. Fundam Clin Pharmacol. 26: 332-9. PMID: 21219440
- Contractile effect of tachykinins on rabbit small intestine. | Valero, MS., et al. 2011. Acta Pharmacol Sin. 32: 487-94. PMID: 21441943
- Substance P inhibits pancreatic ductal bicarbonate secretion via neurokinin receptors 2 and 3 in the guinea pig exocrine pancreas. | Kemény, LV., et al. 2011. Pancreas. 40: 793-5. PMID: 21673544
- High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. | Datta, A., et al. 2018. Sci Rep. 8: 8161. PMID: 29802284
- Prodromal Intestinal Events in Alzheimer's Disease (AD): Colonic Dysmotility and Inflammation Are Associated with Enteric AD-Related Protein Deposition. | Pellegrini, C., et al. 2020. Int J Mol Sci. 21: PMID: 32429301
- Ionic signalling mechanisms involved in neurokinin-3 receptor-mediated augmentation of fear-potentiated startle response in the basolateral amygdala. | Boyle, CA., et al. 2022. J Physiol. 600: 4325-4345. PMID: 36030507
- Dietary Supplement, Containing the Dry Extract of Curcumin, Emblica and Cassia, Counteracts Intestinal Inflammation and Enteric Dysmotility Associated with Obesity. | D'Antongiovanni, V., et al. 2023. Metabolites. 13: PMID: 36984850
- Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. | Giardina, GA., et al. 1997. J Med Chem. 40: 1794-807. PMID: 9191956
Inhibitor of:
NK-3R.Activator of:
NK-3R.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SB 218795, 10 mg | sc-224280 | 10 mg | $193.00 | |||
SB 218795, 50 mg | sc-224280A | 50 mg | $859.00 |