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ABT-670 Sale

目录号 : GC33552

ABT-670是一种具有选择性,可口服的dopamineD4受体抑制剂。

ABT-670 Chemical Structure

Cas No.:630119-43-6

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1mg
¥5,177.00
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5mg
¥10,264.00
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10mg
¥17,493.00
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20mg
¥30,791.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.

ABT-670 is a selective D4 agonist, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively[1].

ABT-670 (0.1 μmol/kg) robustly induces a high (75%) incidence of erections in male rats. ABT-670 exhibits excellent oral bioavailability in rat, dog, and monkey (68%, 85%, and 91%, respectively) with comparable efficacy, safety, and tolerability[1].

[1]. Patel MV, et al. Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction. J Med Chem. 2006 Dec 14;49(25):7450-65.

Chemical Properties

Cas No. 630119-43-6 SDF
Canonical SMILES O=C(NCN1CCC(C2=CC=CC=[N+]2[O-])CC1)C3=CC=CC(C)=C3
分子式 C19H23N3O2 分子量 325.4
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 3.0731 mL 15.3657 mL 30.7314 mL
5 mM 0.6146 mL 3.0731 mL 6.1463 mL
10 mM 0.3073 mL 1.5366 mL 3.0731 mL
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Research Update

Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction

J Med Chem 2006 Dec 14;49(25):7450-65.PMID:17149874DOI:10.1021/jm060662k

The goal of this study was to identify a structurally distinct D(4)-selective agonist with superior oral bioavailability to our first-generation clinical candidate 1a (ABT-724) for the potential treatment of erectile dysfunction. Arylpiperazines such as (heteroarylmethyl)piperazine 1a, benzamide 2, and acetamides such as 3a,b exhibit poor oral bioavailability. Structure-activity relationship (SAR) studies with the arylpiperidine template provided potent partial agonists such as 4d and 5k that demonstrated no improvement in oral bioavailability. Further optimization with the (N-oxy-2-pyridinyl)piperidine template led to the discovery of compound 6b (ABT-670), which exhibited excellent oral bioavailability in rat, dog, and monkey (68%, 85%, and 91%, respectively) with comparable efficacy, safety, and tolerability to 1a. The N-oxy-2-pyridinyl moiety not only provided the structural motif required for agonist function but also reduced metabolism rates. The SAR study leading to the discovery of 6b is described herein.