Naftopidil DiHCl

Catalog No.S1387 Batch:S138701

Technical Data

Formula	C₂₄H₂₈N₂O₃.2HCl
Molecular Weight	465.41	CAS No.	57149-08-3
Solubility (25°C)*	In vitro	DMSO	41 mg/mL (88.09 mM)
		Ethanol	2 mg/mL (4.29 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Naftopidil DiHCl (Flivas, KT-611, Avishot,BM-15275) is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

Targets

5-HT1A ^[1]	α1-adrenergic receptor ^[1]
0.1 μM	0.2 μM

In vitro

Naftopidil diHCl possesses 5-HT1A agonistic properties in addition to being an α1-adrenoceptor antagonist. ^[1] 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 p27^kip1 and p21^cip1 are significantly increased in LNCaP cells treated with Naftopidil. In PC-3 cells, Naftopidil induces p21^cip1 but not p27^kip1. ^[2] 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. ^[3] Naftopidil is significantly more effective than tamsulosin in relieving nocturia. ^[4] 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. ^[5]

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. ^[2] 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). ^[6] Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. ^[7]

Features

Higher selectivity for the -1A and -1D subtypes.

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines LNCaP and PC-3 cell lines Concentrations 20 μM, 40 μM Incubation Time 24 hours Method Cell cycle analysis is performed by flow cytometry. Cells are treated with either 20 μM Naftopidil (LNCaP), 40 μM Naftopidil (PC-3) or vehicle (0.1% DMSO) for 24 hours, then trypsinized and washed once with phosphate-buffer saline (PBS), fixed in 70% ethanol and stored at 4 °C for subsequent cell cycle analysis. Fixed cells are washed with PBS and incubated with PBS containing 20 μg/mL RNaseA and 0.3% NP-40 for 30 minutes at 37 °C, then stained with 50 μg/mL propidium iodide (PI) for 30 minutes at 4 癈 in the dark. The DNA content of 1 ?10⁶ stained cells is analyzed on a FACS Caliburflow cytometer. The fractions of cells in the G0/G1, S and G2/M phases are calculated using Cell Quest software.
Animal Study:^{^[2]}	Animal Models Athymic nude mice bearing PC-3 cells Dosages 10 mL/kg/day Administration Orally

Cell Assay:^{^[2]}

Cell lines
LNCaP and PC-3 cell lines
Concentrations
20 μM, 40 μM
Incubation Time
24 hours
Method
Cell cycle analysis is performed by flow cytometry. Cells are treated with either 20 μM Naftopidil (LNCaP), 40 μM Naftopidil (PC-3) or vehicle (0.1% DMSO) for 24 hours, then trypsinized and washed once with phosphate-buffer saline (PBS), fixed in 70% ethanol and stored at 4 °C for subsequent cell cycle analysis. Fixed cells are washed with PBS and incubated with PBS containing 20 μg/mL RNaseA and 0.3% NP-40 for 30 minutes at 37 °C, then stained with 50 μg/mL propidium iodide (PI) for 30 minutes at 4 癈 in the dark. The DNA content of 1 ?10⁶ stained cells is analyzed on a FACS Caliburflow cytometer. The fractions of cells in the G0/G1, S and G2/M phases are calculated using Cell Quest software.

Animal Study:^{^[2]}

Animal Models
Athymic nude mice bearing PC-3 cells
Dosages
10 mL/kg/day
Administration
Orally

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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