841301-32-4|阿莫奈韦|Amenamevir|MFCD19443709-范德生物科技公司

阿莫奈韦
NMR and HPLC COA下载 MSDS下载
Names：
Amenamevir
CAS号：
841301-32-4
MDL Number： MFCD19443709
MF(分子式)： C24H26N4O5S MW(分子量)： 482.55
EINECS: Reaxys Number:
Pubchem ID:11397521 Brand:BIOFOUNT

阿莫奈韦(841301-32-4,ASP2151,Amenamevir)是一种解旋酶 -primase 抑制剂，对具有EC的HSV具有有效的抗病毒活性₅₀ 14 ng / mL。Amenamevir是一种DNA解旋酶-引发酶抑制剂。它对单纯疱疹性角膜炎具有抗HSV活性。2016年3月，Mahuro在日本完成了单纯疱疹病毒感染的III期试验。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
HCR210343-10mg	10mg	98%	¥ 13300.00	¥ 13300.00		4-7周	- +	¥ 0.00

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中文别名	阿莫奈韦(841301-32-4);阿米那韦;ASP2151;
英文别名	Amenamevir(841301-32-4);amenamevir;UNII-94X46KW4AE; ASP2151; N-(2,6-dimethylphenyl)-N-[2-[4-(1,2,4-oxadiazol-3-yl)anilino]-2-oxoethyl]-1,1-dioxothiane-4-carboxamide;
CAS号	841301-32-4
SMILES	Cc1cccc(c1N(CC(=O)Nc2ccc(cc2)c3ncon3)C(=O)C4CCS(=O)(=O)CC4)C
Inchi	InChI=1S/C24H26N4O5S/c1-16-4-3-5-17(2)22(16)28(24(30)19-10-12-34(31,32)13-11-19)14-21(29)26-20-8-6-18(7-9-20)23-25-15-33-27-23/h3-9,15,19H,10-14H2,1-2H3,(H,26,29)
InchiKey	MNHNIVNAFBSLLX-UHFFFAOYSA-N
分子式 Formula	C24H26N4O5S
分子量 Molecular Weight	482.55
闪点 FP	Not available
熔点 Melting point	Not available
沸点 Boiling point	Not available
Polarizability极化度	49.6±0.5 10-24cm3
密度 Density	1.4±0.1 g/cm3
蒸汽压 Vapor Pressure	Not available
溶解度Solubility	溶于DMSO
性状	粉末
储藏条件 Storage conditions	-20℃冰柜

阿莫奈韦(841301-32-4,ASP2151,Amenamevir)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染
Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	阿莫奈韦(841301-32-4,ASP2151,Amenamevir)可以作为中间体及药物杂质使用，该产品非药用，非食用。
Introduction	阿莫奈韦(841301-32-4,ASP2151only use for non-medical purposes in industrial or scientific research,and not for clinical diagnosis and treatment of humans or animals.This product is not medicinal or edible
Application1	阿莫奈韦是生殖器疱疹豚鼠模型中的疱疹病毒解旋酶-引发酶抑制剂。阿莫奈韦可用于治疗单纯疱疹病毒感染；带状疱疹。
Application2	Amenamevir是一种helicase- primase抑制剂，对具有强效的抗病毒活性的HSV，EC50 约为14 ng / mL。
Application3	Amenamevir是一种解旋酶 -primase 抑制剂，对具有EC的HSV具有有效的抗病毒活性50 14 ng / mL。

阿莫奈韦(841301-32-4,ASP2151,Amenamevir)药理学：

Amenamevir是一种DNA解旋酶-引发酶抑制剂。它对单纯疱疹性角膜炎具有抗HSV活性。2016年3月，Mahuro在日本完成了单纯疱疹病毒感染的III期试验。

Amenamevir是一种新型的解旋酶-引发酶抑制剂，对水痘-带状疱疹病毒和1型和2型单纯疱疹病毒具有活性。干扰病毒DNA复制和病毒生长。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H333吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P313获得医疗建议/护理
备注	Amenamevir实验过程中防止吸入、食入，做好安全防护

Katsumata K, et al. Pharmacokinetics and pharmacodynamics of ASP2151, a helicase-primase inhibitor, in a murine model of herpes simplex virus infection. Antimicrob Agents Chemother. 2013 Mar;57(3):133

Pharmacokinetic Evaluation of the Interactions of Amenamevir (ASP2151) with Ketoconazole, Rifampicin, Midazolam, and Warfarin in Healthy Adults Advances in Therapy 2017 29076107

Pharmacokinetics and Safety of Amenamevir in Healthy Subjects: Analysis of Four Randomized Phase 1 Studies Advances in Therapy 2017 29134426

Pharmacokinetics and Dialyzability of a Single Oral Dose of Amenamevir, an Anti-Herpes Drug, in Hemodialysis Patients Advances in Therapy 2020 32440976

The Influence of Hepatic and Renal Impairment on the Pharmacokinetics of a Treatment for Herpes Zoster, Amenamevir (ASP2151): Phase 1, Open-Label, Single-Dose, Parallel-Group Studies Advances in Thera

阿莫奈韦(841301-32-4,ASP2151,Amenamevir)参考文献：

1.Efficacy of ASP2151, a helicase-primase inhibitor, against thymidine kinase-deficient herpes simplex virus type 2 infection in vitro and in vivo.
Himaki T1, Masui Y, Chono K, Daikoku T, Takemoto M, Haixia B, Okuda T, Suzuki H, Shiraki K. Antiviral Res. 2012 Feb;93(2):301-4. doi: 10.1016/j.antiviral.2011.11.015. Epub 2011 Dec 4.

ASP2151 was developed as a novel inhibitor of herpes simplex virus (HSV) and varicella-zoster virus helicase-primase. The anti-HSV activity of ASP2151 toward a clinical HSV isolate with acyclovir (ACV)-resistant/thymidine kinase (TK)-deficiency was characterized in vitro and in vivo using a plaque reduction assay and the ear pinna infection in mice. The IC(50) ranged from 0.018 to 0.024 μg/ml, indicating the susceptibility of TK-deficient HSV-2 was similar to that of wild-type HSV-2 strains. Anti-HSV activity of ASP2151 in vivo was evaluated in mice infected with wild-type HSV-2 and TK-deficient HSV-2. ASP2151 significantly reduced the copy numbers of wild-type HSV-2 and TK-deficient HSV-2 at the inoculation ear pinna, while valacyclovir significantly reduced the copy number of wild type HSV-2 but not that of TK-deficient HSV-2 in the inoculated ear pinna. Thus, ASP 2151 showed therapeutic efficacy in mice infected with both wild-type and TK-deficient HSV-2.

2、Quantification of ASP2151 in Human Plasma and Urine: A Pitfall Associated with Supersaturation of Analyte in Urine
Yoshiaki Ohtsu, Radboud van Trigt, Kaori Takama, Dorien Groenendaal, Akitsugu Takada, Takeshi Nakamura & Kiyoshi Noguchi

Abstract This is a case study of the difficulties caused by supersaturation of an analyte during the quantification of a drug in urine. To support the clinical development of the potent helicase–primase inhibitor ASP2151, we developed and validated simple and semi-automated methods for determining its concentrations in human plasma and urine. Samples were mixed with an internal standard labeled with stable isotopes, and then filtered. After filtration, the samples were injected into an online extraction, column-switching, liquid chromatography–tandem mass spectrometry analytical system using a validated method. Although quantifiable and reproducible plasma concentrations were obtained with clinical samples, we encountered difficulties with urine samples. Specifically, we found that urinary drug concentrations in some samples ranged between 5 and 67.1 μg mL−1, and exceeded the aqueous saturation concentration (5 μg mL−1), at which dilution integrity was confirmed. In a follow-up experiment using spiked samples, the urine method failed to accurately quantitate ASP2151 concentrations at 10, 25, and 50 µg mL−1 (relative error: −23.5% to −17.2%, coefficient of variation: ≤7.9%). In vitro experiments revealed that urine samples at high ASP2151 concentrations became heterogeneous during sample handling and storage. The problem was solved by revising the sample collection and dilution methods which were subsequently successfully applied to a clinical study.

3、Efficacy of herpes virus helicase-primase inhibitor, ASP2151, for treating herpes simplex keratitis in mouse model
Shin-ichi Sasaki 1, Dai Miyazaki, Tomoko Haruki, Yukimi Yamamoto, Michiko Kandori, Keiko Yakura, Hiroshi Suzuki, Yoshitsugu Inoue

Abstract Aims: To determine the efficacy of a new helicase-primase inhibitor, ASP2151, for treating herpetic keratitis. Methods: Murine corneas were infected with herpes simplex virus type 1 (HSV-1). ASP2151 was administered orally or topically, and the severity of epithelial dendritic keratitis was determined. The effectiveness of ASP2151 was compared with that of acyclovir and valacyclovir. The reduction of the amount of HSV in tears, enucleated eyes and trigeminal ganglia was determined by real-time PCR or plaque assay. Results: Orally administered ASP2151 reduced the epithelial keratitis score significantly more than that of the vehicle-treated group (p<0.01). It also lowered the HSV-DNA levels in the tears significantly more than that by valacyclovir (p<0.01). ASP2151 ointment resulted in the same reduction of the keratitis score as acyclovir ointment, and lowered the HSV DNA in tears more than acyclovir ointment. Topical instillation of ASP2151 improved the herpetic dendritic keratitis score significantly and reduced the titre of HSV DNA in the tears in a dose-responsive way. Conclusions: ASP2151 had significantly better anti-HSV activity against herpes simplex keratitis than valacyclovir and acyclovir after systemic or topical use. These findings indicate that ASP2151 should be considered as an alternative treatment for herpes simplex keratitis.

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