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Naftopidil

Catalog No. T0696 CAS 57149-07-2

Synonyms: KT-611, BM-15275

Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.

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Naftopidil, CAS 57149-07-2

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500 mg	In stock	$ 41.00
1 g	In stock	$ 66.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.4%

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Storage & Solubility Information

Description	Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.
Targets&IC50	α1B-adrenoceptor:20 nM(Ki), α1A-adrenoceptor:3.7 nM(Ki), α1D-adrenoceptor:1.2 nM(Ki)
In vitro	Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. [1] 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. [2] 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. [3] 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. [4] 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. [5]
In vivo	Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. [1] Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats. [5]

Synonyms	KT-611, BM-15275
Molecular Weight	392.49
Formula	C24H28N2O3
CAS No.	57149-07-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 73 mg/mL (186 mM)

References and Literature

1. Takei R, et al. Jpn J Pharmacol,1999, 79(4), 447-454. 2. Kanda H, et al. Int J Cancer,2008, 122(2), 444-451. 3. Masachika E, et al. Anticancer Res,2013, 33(3), 887-894. 4. Alarayyed NA, et al. Br J Clin Pharmacol,1997, 43(4), 415-420. 5. Sakai T, et al. Eur J Pharmacol,2013, 700(1-3), 194-200.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Obesity Compound Library ReFRAME Related Library

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Keywords

Naftopidil 57149-07-2 GPCR/G Protein Neuroscience Adrenergic Receptor hyperplasia BM 15275 KT-611 inhibit prostate pressure BM15275 KT 611 canine Inhibitor BM-15275 KT611 Beta Receptor prostatic inhibitor

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