Product Details
Product Name:
Naluzotan |
CAS No.:
740873-06-7 |
Purity:
100% |
Supply Ability:
10g |
Release date:
2024/11/20 |
Product Introduction
Bioactivity
Name | Naluzotan |
Description | Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression. |
In vitro | Naluzotan, with an EC50 of 20 nM, behaves as a full agonist in an in vitro cell-based functional assay. It exhibits significant affinity for the guinea pig sigma receptor (Ki = 100 nM) but does not inhibit cytochrome P450 isoforms (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4[2]. |
In vivo | In rats, when administered orally, Naluzotan shows 11% oral bioavailability with a serum half-life (t1/2) of 2?3.5 hours, reaching a Cmax level of 24 ± 13 ng/mL (3 mg/kg, oral). Naluzotan exhibits significant brain penetration, with a brain:serum concentration ratio of approximately 0.5 in rats at 1 hour following either intravenous or oral administration, and it achieves a brain concentration approximately equivalent to that of buspirone. In dogs, the pharmacokinetic profile of naluzotan demonstrates 16% oral bioavailability, a serum t1/2 of 1.1 hours when administered orally, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, oral)[1]. PRX-00023, at doses of 0.01-0.05 mg/kg administered intraperitoneally, significantly reduces ultrasonic vocalization (USV) rates in rats, but none of these doses induce sedation[1]. |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Keywords | PRX00023 | PRX-00023 | Naluzotan |
Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | Osimertinib | CLOZAPINE N-OXIDE | Lapatinib | Erlotinib | Neratinib | Genistein | Gefitinib | Trazodone hydrochloride |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries, 10000+ Noval Small Molecucles,16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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Recommended supplier
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Price |
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Suppliers |
Update time |
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$230.00/1mg |
VIP5Y
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TargetMol Chemicals Inc.
|
2024-11-19 |