| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N408047-1ml |
1ml |
现货  |
|
| 英文别名 | KT-611 | 4-(2-methoxyphenyl)-α-[(1-naphthalenyloxy)methyl]-1-piperazineethanol |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Naftopidil |
| 生化机理 | 萘夫地尔（KT-611）是一种选择性α1-肾上腺素能受体拮抗剂，对α1a、α1b和α1d的Ki分别为3.7 nM、20 nM和1.2 nM，用于治疗良性前列腺增生。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | α-1d肾上腺素能受体拮抗剂 |
| 产品介绍 |
Naftopidil 是选择性α1-肾上腺素能受体拮抗剂，或α受体抑制剂，Ki为58.3 nM。N α-1-Adrenergic receptor antagonist and an antihypertensive. Information Naftopidil (KT-611) is a selectiveα1-adrenergic receptorantagonist withKiof 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia. Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil induces p21(cip1) but not p27(kip1) in PC-3 cells. Naftopidil induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Naftopidil-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. Naftopidil, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM Naftopidil. Naftopidil also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. Naftopidil (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. Naftopidil inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. Naftopidil binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively. In vivo Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats. cell lines：Human monocytes Concentrations： Incubation Time： Powder Purity:≥98% |
| Ki Data | α1D-adrenergic receptor, Ki: 1.2 nM; α1A-adrenergic receptor, Ki: 3.7 nM; α1B-adrenergic receptor, Ki: 20 nM |
|---|---|
| ALogP | 3.962 |
| hba_count | 2 |
| HBD Count | 1 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC=CC=C1N2CCN(CC2)CC(O)COC3=C4C=CC=CC4=CC=C3 |
| 分子量 | 392.49 |
| Reaxy-Rn | 629965 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=629965&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 33 mg/mL (198.53 mM); Water: 33 mg/mL warmed with 50ºC Water: bath (198.53 mM); Ethanol: 33 mg/mL (198.53 mM); |
|---|---|
| DMSO(mg / mL) Max Solubility | 79 |
| DMSO(mM) Max Solubility | 201.28 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 629965 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=629965&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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