Home>>Signaling Pathways>> Metabolism>> HSP>>Icapamespib

Icapamespib Sale

(Synonyms: PU-HZ151) 目录号 : GC63282

Icapamespib (PU-HZ151) 是一种有效的 HSP90 抑制剂,EC50 值为5 nM. Icapamespib 可以透过血脑屏障。

Icapamespib Chemical Structure

Cas No.:1000999-96-1

规格 价格 库存 购买数量
5 mg
¥4,050.00
现货
10 mg
¥7,200.00
现货
25 mg
¥14,850.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

Icapamespib (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib is able to cross blood-brain barrier[1].

[1]. Bolaender A, et al. Chemical tools for epichaperome-mediated interactome dysfunctions of the central nervous system. Nat Commun. 2021;12(1):4669. Published 2021 Aug 3.

Chemical Properties

Cas No. 1000999-96-1 SDF
别名 PU-HZ151
分子式 C19H23IN6O2S 分子量 526.39
溶解度 储存条件 Store at -20°C
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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.8997 mL 9.4987 mL 18.9973 mL
5 mM 0.3799 mL 1.8997 mL 3.7995 mL
10 mM 0.19 mL 0.9499 mL 1.8997 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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

Research Update

Safety, Tolerability and Pharmacokinetics of Icapamespib, a Selective Epichaperome Inhibitor, in Healthy Adults

J Prev Alzheimers Dis 2022;9(4):635-645.PMID:36281667DOI:PMC9419134

Background: Neurodegenerative diseases are devastating conditions that most commonly affect individuals 65 years and older. Currently there are no effective treatments or cures for neurodegenerative diseases, and therapeutics that selectively target the underlying causes of these diseases are needed. Epichaperomes play a major role in the maintenance and progression of neuronal pathology. Inhibiting epichaperomes induces degradation of disease associated proteins and is a promising therapeutic approach to treat neurodegenerative diseases, in particular Alzheimer's Disease and amyotrophic lateral sclerosis. Objectives: This Phase 1 clinical study evaluated the safety, tolerability, pharmacokinetics, and bioavailability of Icapamespib, a purine scaffold inhibitor of epichaperomes that is specific to epichaperomes, in healthy subjects. Design: Double-blind, placebo-controlled dose escalating single ascending dose and multiple ascending doses and an unblinded two-period cross-over bioavailability study design. Setting: Single site in the United States. Participants: Healthy men or women of 18 to 60 years of age, inclusive, for Part 1 (single ascending dose), ≥ 60 years of age for Part 2 (multiple ascending dose), or 18 to 49 years of age for Part 3 (bioavailability). Treatment: In the single ascending dose group, oral single doses (10, 20, and 30 mg Icapamespib or placebo) were administered to healthy non-elderly subjects. In the multiple ascending dose group, multiple doses (20 and 30 mg Icapamespib once daily for 7 days or placebo) were administered to healthy elderly subjects. In the bioavailability group, the bioavailability of once daily oral Icapamespib solution and tablet was assessed in healthy non elderly subjects. Measurements: Safety was evaluated based on assessments of treatment-emergent adverse events, physical examinations, clinical laboratory tests (hematology, clinical chemistry, and urinalysis), vital signs, and 12-lead electrocardiograms. Icapamespib concentration was evaluated in plasma and cerebrospinal fluid, the latter in Part 2 (multiple ascending dose) only. Results: Forty-eight subjects in total were randomized and assessed for tolerability, pharmacokinetics, and bioavailability parameters as follows: 24 subjects in Part 1 (single ascending dose) with PU-AD 10 mg (n = 6), 20 mg (n = 6), 30 mg (n = 6), and placebo (n = 6); 16 subjects in Part 2 (multiple ascending dose) with Icapamespib 20 mg (n = 6), 30 mg (n = 6), and placebo (n = 4); and 8 subjects in Part 3 (bioavailability) crossed-over between Icapamespib 30 mg (tablet) and Icapamespib 30 mg (oral solution). Single doses of Icapamespib up to 30 mg and multiple doses of Icapamespib up to 30 mg for 7 days were generally safe and well tolerated in healthy non-elderly and elderly subjects. Treatment-emergent adverse events were mild, with headache being the most common treatment-emergent adverse event. Mean Icapamespib exposure (area under the curve) was dose-proportional over the dose range tested. The median time to maximum observed plasma concentration ranged from 1.00 to 2.00 h across single ascending dose, multiple ascending dose, and bioavailability groups; Icapamespib exposure was 50% higher in elderly subjects compared with non-elderly subjects but was well tolerated. Conclusions: The study provides clinical evidence of the safety of Icapamespib in healthy non elderly and elderly subjects and supports the advancement of Icapamespib to Phase 2 evaluation in Alzheimer's Disease and other neurodegenerative diseases.