Abametapir
(Synonyms: 55'-二甲基-2,2-联吡啶) 目录号 : GC46769
A building block and an insecticide
Cas No.:1762-34-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Abametapir is a building block and an insectide.1,2,3 It has been used in the synthesis of lanthanide coordination complexes with antifungal activity against C. albicans and divalent vancomycin derivatives with antibacterial activity against vancomycin-resistant enterococci.1,2 Abametapir is ovicidal to DDT- and permethrin-resistant head louse eggs (LC50s = 0.108, 0.121, and 0.16% in isopropanol for 0-2-, 3-5-, and 6-8-day-old eggs, respectively).3 Formulations containing abametapir have been used in the topical treatment of head lice infestation.
1.Zhou, M.-X., Ren, N., Zhang, J.-J., et al.Synthesis, crystal structure, thermal, luminescent property and antibacterial activity of lanthanide ternary complexes with p-chlorobenzoic acid and 5,5′-dimethyl-2,2′-bipyridineJ. Mol. Struct.1200127049(2020) 2.Xing, B., Yu, C.-W., Ho, P.-L., et al.Multivalent antibiotics via metal complexes: Potent divalent vancomycins against vancomycin-resistant enterococciJ. Med. Chem.46(23)4904-4909(2003) 3.Bowles, V.M., Yoon, K.S., Barker, S.C., et al.Ovicidal efficacy of abametapir against eggs of human head and body lice (Anoplura: Pediculidae)J. Med. Entomol.54(1)167-172(2017)
| Cas No. | 1762-34-1 | SDF | |
| 别名 | 55'-二甲基-2,2-联吡啶 | ||
| Canonical SMILES | CC1=CC=C(C2=CC=C(C)C=N2)N=C1 | ||
| 分子式 | C12H12N2 | 分子量 | 184.2 |
| 溶解度 | DMF: 15mg/mL,DMSO: 10mg/mL,Ethanol: 15mg/mL,Ethanol:PBS (pH 7.2) (1:4): 0.2mg/mL | 储存条件 | 4°C, protect from light, stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.4289 mL | 27.1444 mL | 54.2888 mL |
| 5 mM | 1.0858 mL | 5.4289 mL | 10.8578 mL |
| 10 mM | 0.5429 mL | 2.7144 mL | 5.4289 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Abametapir for the Treatment of Head Lice: A Drug Review
Ann Pharmacother 2022 Mar;56(3):352-357.PMID:34157881DOI:10.1177/10600280211027968.
Objective: This article reviews the pharmacology, safety, efficacy, and clinical importance of Abametapir 0.74% (Xeglyze) for the treatment of head lice. Data sources: From 2020 to May 2021, a systematic review of the MEDLINE and EMBASE databases was conducted using the terms Abametapir, Xeglyze, Ha44, and head lice. Bibliographies, Food and Drug Administration (FDA) drug package inserts, and ClinicalTrials.gov were searched for further information. Study selection and data extraction: All relevant full-text articles in English were considered for inclusion, with a final article date range of 1999 to 2020. Data synthesis: Abametapir chelates heavy metal cations and inhibits metalloproteinases critical to louse ova development, hatching, and adult survival. In phase II, Abametapir had direct ovicidal activity inhibiting 100% of treated louse eggs from hatching, compared with 64% in the vehicle-treated group. In two identical phase III clinical trials, subjects treated with a single 10-minute application of Abametapir had greater treatment success compared with vehicle-treated subjects, with 81.1% success versus 50.9% in study 1 (P = 0.001) and 81.8% versus 47.2% in study 2 (P < 0.001). Abametapir was well tolerated, with only mild adverse effects. Relevance to patient care and clinical practice: Abametapir is a newly FDA-approved, single-application treatment for head lice in patients aged 6 months and older. This review highlights the safety and efficacy of Abametapir in the treatment of head lice. Conclusions: In the wake of increasing widespread resistance to first-line treatment options, Abametapir offers a safe and effective new treatment option for head lice infestations.
Abametapir 0.74% (Xeglyze) for the Treatment of Head Lice
Am Fam Physician 2022 Jul;106(1):91-92.PMID:35839355doi
Abametapir 0.74% (Xeglyze) is a topical ovicidal pediculicide labeled for the treatment of head lice infestation in patients six months and older.1,2.
Common pediatric infestations: update on diagnosis and treatment of scabies, head lice, and bed bugs
Curr Opin Pediatr 2021 Aug 1;33(4):410-415.PMID:34074914DOI:10.1097/MOP.0000000000001031.
Purpose of the review: This review will update pediatric providers on the recent data regarding the epidemiology, diagnosis, and treatment of common skin infestations affecting children and adolescents. Recent findings: Standard superficial skin biopsy for scabies and the vacuum method for head lice can increase diagnostic accuracy and efficiency. There is growing resistance to some of the traditional treatments for scabies and head lice, and progress has been made in finding newer and potentially more effective treatments, such as oral moxidectin for scabies and Abametapir for head lice. Recent studies have established the safety of traditional treatments, such as permethrin and oral ivermectin in infants and small children. Summary: Permethrin and ivermectin are both considered safe and effective for children and adolescents with scabies. Permethrin is generally considered safe in infants less than two months of age. Proper application of permethrin is critical, and providers should emphasize proper application technique. Treatment of head lice should only be initiated with active infestations. Resistance to permethrin continues to increase and other options are now available, including an over-the-counter topical ivermectin formulation. Identification and eradication of bed bug infestations are crucial in preventing bedbug bites.
Clinical studies evaluating Abametapir lotion, 0.74%, for the treatment of head louse infestation
Pediatr Dermatol 2018 Sep;35(5):616-621.PMID:29999197DOI:10.1111/pde.13612.
Background: There is a need for better control of head louse infestations. Abametapir is an inhibitor of metalloproteinases critical for louse survival and egg development. The efficacy of Abametapir lotion, 0.74%, was assessed for its ability to clear head louse infestations after a single application. Methods: Two randomized, double-blind, multicenter, vehicle-controlled studies were conducted in subjects aged 6 months and older to compare the effectiveness of Abametapir lotion versus vehicle control for eliminating head louse infestations without nit combing. Abametapir lotion was applied to dry hair for 10 minutes on day 0 and then rinsed with water. The primary endpoint was the proportion of index subjects (youngest household member with ≥ 3 live lice at screening) in the intent-to-treat population who were louse free at all follow-up visits through day 14. Older household members with one or more live lice at screening were designated as nonindex subjects and treated as per the index subject within their household. Results: In the intent-to-treat population (index subjects, N = 216), 81.5% of subjects treated with Abametapir lotion were louse free through day 14 after a single treatment, versus 49.1% with vehicle (P < 0.001). For the combined index and nonindex population (N = 704), 85.9% were louse free through day 14 in the Abametapir group, versus 61.3% in the vehicle group (P < 0.001). The most frequently reported adverse events were erythema (4.0%), rash (3.2%), and skin burning sensation (2.6%). Conclusion: Abametapir lotion, 0.74%, was effective at clearing active head louse infestations through day 14 in subjects aged 6 months and older. All adverse events (including one serious but unrelated to study drug) resolved uneventfully.
Ovicidal Efficacy of Abametapir Against Eggs of Human Head and Body Lice (Anoplura: Pediculidae)
J Med Entomol 2017 Jan;54(1):167-172.PMID:28082644DOI:10.1093/jme/tjw132.
Studies were undertaken to determine the ovicidal efficacy of 5,5'-dimethyl-2,2'-bipyridyl (Abametapir) against eggs of both human head and body lice. Head lice eggs of different ages (0-2, 3-5, and 6-8-d-old eggs) were exposed to varying concentrations of Abametapir in isopropanol and concentration-dependent response relationships established based on egg hatch. One hundred percent of all abametapir-treated eggs failed to hatch at the 0.74 and 0.55% concentrations, whereas 100% of 6-8-d-old head louse eggs failed to hatch only at the 0.74% concentration. The LC50 value for Abametapir varied, depending on the age of the head lice eggs, from ∼0.10% recorded for 0-2-d-old eggs and increasing to ∼0.15% for 6-8-d-old eggs. Abametapir was also evaluated once formulated into a lotion referred to as Xeglyze (0.74% Abametapir) and serial dilutions made. Ovicidal efficacies were determined against head lice eggs 0-8-d-old. Results indicated 100% ovicidal activity at the 0.74, 0.55, 0.37, and 0.18% concentrations. Additional studies undertaken using body lice eggs also demonstrated that Abametapir was 100% ovicidal against eggs of all ages when evaluated at a concentration of 0.37 and 0.55%. Given that ovicidal activity is a critical component of any effective treatment regime for louse control, the data presented in this study clearly demonstrate the ability of Abametapir to inhibit hatching of both head and body louse eggs as assessed in vitro.