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My CartCAS：57149-07-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 57149-07-2 |
| Name | Naftopidil |
| Molecular Formula | C24H28N2O3 |
| Molecular Weight | 392.49 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00242741 |
| SMILES | COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O |
| InChIKey | HRRBJVNMSRJFHQ-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H28N2O3/c1-28-24-11-5-4-10-22(24)26-15-13-25(14-16-26)17-20(27)18-29-23-12-6-8-19-7-2-3-9-21(19)23/h2-12，20，27H，13-18H2，1H3 |
| PubChem CID | 4418 |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein；Neuronal Signaling |
| Background | It is a selective alpha1- adrenoceptor antagonist. |
| Biological Activity | Naftopidil 是一种选择性α1-肾上腺素受体拮抗剂，对克隆的人类α1a-、α1b-和α1d-肾上腺素受体亚型的 Kis 值分别为 3.7 nM、20 nM 和 1.2 nM。Naftopidil 具有抑制细胞增殖的作用。[1-2] |
| In Vitro | Naftopidil selectively inhibited the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes，respectively.[1] Naftopidil(10 μM; 3 days)showed antiproliferative effects on PCa cells. In PrSC，a strong growth inhibitory effect was observed with naftopidil(0.1-10 μM for PrSC; 3 days). Naftopidil induced G(1)cell-cycle arrest in both PCa cells and PrSC.[2] |
| In Vivo | Tumorigenic studies in vivo showed significant reductions in tumor growth when E9 cells(an androgen low-sensitive LNCaP subline)grafted with PrSC were treated with naftopidil(10 mg/kg; p.o; daily; for 28 days).[2] |
| Data Literature Source | [1]. Takei R，et al. Naftopidil，a novel alpha1-adrenoceptor antagonist，displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol. 1999 Apr;79(4):447-54. [2]. Hori Y，et al. Naftopidil，a selective {alpha}1-adrenoceptor antagonist，suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Cancer Prev Res (Phila). 2011 Jan;4(1):87-96. |
| Unit | Bottle |
| Specification | 250mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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