计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Naftopidil DiHCl是一种选择性5-HT1A和α1-adrenergic receptor（α1-肾上腺素受体）拮抗剂，IC50分别为0.1 μM和0.2 μM。
Information
Naftopidil DiHCl (KT-611) is a selective5-HT1Aandα1-adrenergic receptorantagonist withIC50of 0.1 μM and 0.2 μM, respectively.
In vitro
Naftopidil diHCl possesses 5-HT1A agonistic properties in addition to being an α1-adrenoceptor antagonist. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil inhibits the growth of androgen-sensitive LNCaP cells and androgen-insensitive PC-3 cells with IC50 of 22.2 μM and 33.2 μM, respectively. Cell growth inhibition by Naftopidil is due to the arrest of the G1 cell cycle. Expressions of p27kip1 and p21cip1 are significantly increased in LNCaP cells treated with Naftopidil. In PC-3 cells, Naftopidil induces p21cip1 but not p27kip1. Naftopidil produces a concentration-dependent inhibition of collagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 μM Naftopidil. The adrenaline-induced rise in [Ca2+]i is inhibited dose dependently by Naftopidil. Naftopidil is significantly more effective than tamsulosin in relieving nocturia. Naftopidil induces G(1) cell-cycle arrest in both PCa cells and PrSC. In Naftopidil-treated PrSC, total interleukin-6 protein is significantly reduced with increased suppression of cell proliferation.
In vivo
Oral administration of Naftopidil to nude mice inhibits the growth of PC-3 tumors as compared to vehicle-treated controls. Naftopidil improves bladder capacity and relaxed voiding via inhibition of afferent nerve activity. Naftopidil (0.1 μg–30 μg) transiently abolishes isovolumetric rhythmic bladder contraction. The amplitude of bladder contraction is decreased by intrathecal injection of naftopidil (3 μg–30 μg). Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model.
Cell Data
cell lines：BT474, HT1376, UMUC-3, T24, ACHN, DU-145, PC-3, LN-REC4, and LNCaP cells
Concentrations：20 μM, 40 μM
Incubation Time：24 hours
Powder Purity:≥99%
规格
英文别名
KT-611 | 1-(4-(2-methoxyphenyl)piperazin-1-yl)-3-(naphthalen-1-yloxy)propan-2-ol dihydrochloride
规格或纯度
10mM in DMSO
英文名称
Naftopidil DiHCl
生化机理
Naftopidil DiHCl（KT-611）是一种选择性 5-HT1A 和 α1 肾上腺素能受体拮抗剂，IC50 分别为 0.1 μM 和 0.2 μM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O.Cl.Cl
PubChem CID
分子量
465.41
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro 0.5MNAOH 3.02 mg/mL (17.96 mM); DMSO: 0.01 mg/mL (0.05 mM); Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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