| 货号 | 19551-100mg |
| 描述 | Cyproheptadine is a first-generation antihistamine that potently antagonizes the histamine H1 receptor (pKi = 9.42).1,2 It also antagonizes serotonin and muscarinic receptors at nanomolar concentrations.3,4 Cyproheptadine also inhibits the lysine methyltransferase SET7/9 (IC50 = 1 µM), suppressing the expression of estrogen receptor α in human breast cancer MCF-7 cells.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kakiuchi, M.,Ohashi, T.,Musoh, K., et al. Studies on the novel antiallergic agent HSR-609: Its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor. Japanese Journal of Pharmacology 73(4), 291-298 (1997). 2.ter Laak, A.M.,Venhorst, J.,Donné-Op den Kelder, G.M., et al. The histamine H1-receptor antagonist binding site. A stereoselective pharmacophoric model based upon (semi-)rigid H1-antagonists and including a known interaction site on the receptor. Journal of Medicinal Chemistry 38, 3351-3360 (1995). 3.Honda, M.,Nishida, T. and Ono, H. Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT2 receptors. European Journal of Pharmacology 458(1-2), 91-99 (2003). 4.Stanton, T.,Bolden-Watson, C.,Cusack, B., et al. Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics. Biochemical Pharmacology 45(11), 2352-2354 (1993). 5.Takemoto, Y.,Ito, A.,Niwa, H., et al. Identification of cyproheptadine as an inhibitor of SET domain containing lysine methyltransferase 7/9 (Set7/9) that regulates estrogen-dependent transcription. Journal of Medicinal Chemistry 59(8), 3650-3660 (2016). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 287.4 |
| 分子式 | C21H21N |
| CAS号 | 129-03-3 |
| 稳定性 | ≥ 2 years |
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