Tepilamide fumarate
(Synonyms: XP-23829; PPC-06) 目录号 : GC37764
Tepilamide fumarate (XP-23829) 是一种延胡索酸酯，可用于中度到重度慢性斑块银屑病的研究。
Cas No.:1208229-58-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tepilamide fumarate (XP-23829) is an oral fumaric acid ester, acts as a prodrug of monomethyl fumarate, and is used in the research of moderate to severe chronic plaque psoriasis[1].
[1]. Dr. Reddy's Laboratories and XenoPort Enter Into a U.S. Licensing Agreement for XP23829.
| Cas No. | 1208229-58-6 | SDF | |
| 别名 | XP-23829; PPC-06 | ||
| Canonical SMILES | O=C(OCC(N(CC)CC)=O)/C=C/C(OC)=O | ||
| 分子式 | C11H17NO5 | 分子量 | 243.26 |
| 溶解度 | DMSO: ≥ 125 mg/mL (513.85 mM) | 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。 |
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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 | 4.1108 mL | 20.5541 mL | 41.1083 mL |
| 5 mM | 0.8222 mL | 4.1108 mL | 8.2217 mL |
| 10 mM | 0.4111 mL | 2.0554 mL | 4.1108 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。
Tepilamide fumarate (PPC-06) Extended Release Tablets in Patients with Moderate-to-Severe Plaque Psoriasis: Safety and Efficacy Results from the Randomized, Double-blind, Placebo-controlled AFFIRM Study
J Clin Aesthet Dermatol 2022 Jan;15(1):53-58.PMID:35309277DOI:PMC8903235
Objective: Safe, effective, long-term oral therapies are needed for plaque psoriasis. This study aimed to assess the safety and effectiveness of Tepilamide fumarate (a fumaric acid ester) extended-release tablets. Methods: This Phase IIb, randomized, double-blind, placebo-controlled, 24-week, multicenter study treated adults with moderate-to-severe plaque psoriasis with Tepilamide fumarate 400 mg once (QD) or twice daily (BID), 600 mg BID, or placebo. Coprimary endpoints were the proportion of patients achieving ≥75% reduction in the Psoriasis Area and Severity Index (PASI-75) and Investigator's Global Assessment (IGA) of clear or almost clear (≥2 points' reduction). Results: A total of 426 patients were randomized (mean age 49.6 [±13.0] years). There was a ≥75% PASI reduction in 39.7%, 47.2%, 44.3%, and 20.0% in the 400 mg QD, 400 mg BID, 600 mg BID, and placebo groups, respectively; IGA treatment success was 35.7%, 41.4%, 44.4%, and 22.0%, respectively. Between 50%-66% of Tepilamide fumarate and 48% of placebo patients experienced ≥1 treatment-emergent adverse event. Gastrointestinal intolerance (20%-42%), infection (6%-18%), and decreased lymphocyte count (4%-9%) were more common with Tepilamide fumarate. Limitations: High placebo response somewhat limits the utility of these findings. Conclusion: Patients with moderate-to-severe plaque psoriasis treated with oral Tepilamide fumarate demonstrated positive response.