Trifarotene (CD5789)
(Synonyms: 曲法罗汀; CD5789) 目录号 : GC31935
Trifarotene (CD5789) (CD5789) 是一种有效的选择性 RARγ；激动剂。
Cas No.:895542-09-3
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
Trifarotene is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
[1]. Thibaud Biadatti, et al. Novel ligands that modulate rar receptors, and use thereof in human medicine and in cosmetics. WO 2006066978 A1.
| Cas No. | 895542-09-3 | SDF | |
| 别名 | 曲法罗汀; CD5789 | ||
| Canonical SMILES | O=C(C1=CC=C(C2=CC=C(OCCO)C(C3=CC=C(N4CCCC4)C(C(C)(C)C)=C3)=C2)C=C1)O | ||
| 分子式 | C29H33NO4 | 分子量 | 459.58 |
| 溶解度 | DMSO: 250 mg/mL (543.97 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 | 2.1759 mL | 10.8795 mL | 21.759 mL |
| 5 mM | 0.4352 mL | 2.1759 mL | 4.3518 mL |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1759 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。
New Developments in Topical Acne Therapy
Acne vulgaris is a common chronic inflammatory disease with a multifactorial pathogenesis. Although myriad acne treatments are available, current options may not be sufficient because of a lack of efficacy, limited tolerability, or burden of cost to patients. In this review, we highlight recently approved topical acne treatments, as well as those currently in clinical trials. Novel formulations of tretinoin, tazarotene, and minocycline provide modifications of and improvements to existing products. Trifarotene, a novel fourth-generation retinoid, has demonstrated improved tolerability compared with existing topical retinoids. Clascoterone is a novel first-in-class antiandrogen that topically addresses the hormonal etiology of acne. The late-phase clinical trials pipeline consists of agents with bactericidal and anti-sebum mechanisms. Although it is evident that acne treatments continue to evolve, it is important to recognize the need for further comparative studies among new and existing agents to define optimal treatment algorithms that address not only safety and efficacy but also cost-effective care.
New Acne Therapies and Updates on Use of Spironolactone and Isotretinoin: A Narrative Review
Acne vulgaris is a chronic inflammatory skin disease with a multifactorial pathogenesis. Although a variety of acne treatments are available, limitations of current therapies include tolerability, antimicrobial resistance, and costs and patient burden associated with monitoring. This narrative review focuses on emerging treatments and updates on the management of acne. Clascoterone, sarecycline, trifarotene, and novel lotion formulations of tretinoin and tazarotene have been evaluated in clinical trials and provide new options for treatment. Emerging data on the safety and efficacy of spironolactone and isotretinoin challenge current conventions and suggest a need to reconsider drug monitoring guidelines and risk prevention systems. Additional head-to-head data are needed to confirm these novel treatments' utility in treating acne.
Trifarotene
Trifarotene has not been studied during breastfeeding. Because it is poorly absorbed after topical application, it is a low risk to the nursing infant. Do not apply trifarotene cream directly to the nipple and areola and ensure that the infant's skin does not come into direct contact with the areas of skin that have been treated.
Trifarotene for acne
50 Years of Topical Retinoids for Acne: Evolution of Treatment
Since the US Food and Drug Administration (FDA) approved tretinoin in 1971, retinoids alone or combined with other agents have become the mainstay of acne treatment. Retinoids act through binding to retinoic acid receptors, altering expression levels of hundreds of cellular proteins affecting multiple pathways involved in acne pathogenesis. Retinoids have evolved from first-generation agents, such as tretinoin, through chemical modifications resulting in a second generation (etretinate and acitretin for psoriasis), a third generation (adapalene and tazarotene) and, most recently, a fourth (trifarotene). For all topical retinoids, local irritation has been associated with poor tolerability and suboptimal adherence. Efforts to improve tolerability have utilized novel delivery systems and/or novel agents. This qualitative literature review summarizes the evolution of the four topical single-agent retinoids available for the treatment of acne in the US today and their various formulations, presenting the rationale behind their development and data from key studies.