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- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Cyproheptadine Hydrochloride Sesquihydrate
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
41354-29-4
- 规格：
100mg/200mg/500mg/1g/5g
| 规格： | 100mg | 产品价格： | ¥110.00 |
|---|---|---|---|
| 规格： | 200mg | 产品价格： | ¥140.00 |
| 规格： | 500mg | 产品价格： | ¥188.00 |
| 规格： | 1g | 产品价格： | ¥220.00 |
| 规格： | 5g | 产品价格： | ¥270.00 |
| CAS | 41354-29-4 |
| 中文名称 | 盐酸赛庚啶倍半水合物 |
| 英文名称 | Cyproheptadine Hydrochloride Sesquihydrate |
| 别名 | Periactin hydrochloride;Peritol;Cyproheptadine hydrochloride sesquihydrate;盐酸赛庚啶半水合物 |
| 分子式 | C21H21N·3/2H2O·HCl |
| 分子量 | 350.88 |
| 规格 | 100mg ; 200mg ; 500mg ; 1g ; 5g |
| 溶解性 | Soluble in DMSO ≥3mg/mL |
| 纯度 | ≥98% |
| 级别 | Cell Culture |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | EINECS 213-535-1 |
| MDL | MFCD00012538 |
| SMILES | CN1CCC(=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1.CN1CCC(=C2C3=CC=CC=C3C=CC4=CC=CC=C42)CC1.O.O.O.Cl.Cl |
| InChIKey | ZEAUHIZSRUAMQG-UHFFFAOYSA-N |
| InChI | InChI=1S/2C21H21N.2ClH.3H2O/c2*1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21;;;;;/h2*2-11H，12-15H2，1H3;2*1H;3*1H2 |
| PubChem CID | 11954233 |
| 靶点 | 5-HT Receptor;SETD7/9 |
| 通路 | Neuronal Signaling；GPCR & G Protein;Epigenetics |
| 背景说明 | 是非选择性的5HT2拮抗剂;也是SETD7/9的抑制剂。 |
| 生物活性 | Cyproheptadine Hydrochloride 是一种非选择性的 5HT2 受体拮抗剂，其IC50为0.6 nM，也是一种 SETD7/9 抑制剂。[1-3] |
| IC50 | 5-HT2: 0.6nM(IC50)[1];SETD7/9: 1μM(IC50)[3] |
| In Vitro | Subthreshold concentration of 5-HT(2 micromol/L)potentiated the effect of low dose of arachidonic acid(AA)(0.2 mmol/L)in human platelets. This synergistic effect was blocked by 5-HT2 receptor antagonist(cyproheptadine IC(50)=0.6 nmol/L).[1] Cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. Treatment of human breast cancer cells(MCF7 cells)with cyproheptadine decreased the expression and transcriptional activity of ERα，thereby inhibiting estrogen-dependent cell growth.[3] |
| In Vivo | Cyproheptadine significantly inhibited facilitatory effects of 1-(2，5-dimethoxy-4-iodophenyl)-2-aminopropane(DOI)on flexor reflexes and mono- and polysynaptic spinal reflex potentials in spinalized rats.[2] |
| 细胞实验 | Treatment of human breast cancer cells(MCF7 cells)with cyproheptadine decreased the expression and transcriptional activity of ERα，thereby inhibiting estrogen-dependent cell growth. [3] |
| 激酶实验 | Kinetic and X-ray crystallographic analyses revealed that cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. [3] |
| 数据来源文献 | [1]. Saeed SA，et al. Synergism interaction between arachidonic acid by 5-hydroxytryptamine in human platelet aggregation is mediated through multiple signalling pathways. Acta Pharmacol Sin. 2003 Oct;24(10):958-64. [2]. Honda M，et al. Tricyclic analogs cyclobenzaprine，amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9. [3]. Takemoto Y，et al. Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. J Med Chem. 2016 Apr 28;59(8):3650-60. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.85mL|14.2499mL|28.4998mL|$$|5mM|0.57mL|2.85mL|5.7mL|$$|10mM|0.285mL|1.425mL|2.85mL| |
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盐酸赛庚啶倍半水合物
¥110 - 270
