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Cintirorgon
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cintirorgon图片
CAS NO:2055536-64-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
LYC-55716
产品介绍
Cintirorgon (LYC-55716) 是一种首创的、选择性的,具有口服活性的RORγ激动剂。Cintirorgon (LYC-55716) 调节 RORγ 表达的 T 淋巴细胞免疫细胞的基因表达,增强效应子功能,降低免疫抑制,降低肿瘤生长,提高生存率 。
生物活性

Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailableRORγagonist. Cintirorgon (LYC-55716) modulates gene expression ofRORγexpressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival[1][2].

IC50& Target

RORγ[1]

体内研究
(In Vivo)

Upon oral administration of RORγ agonist Cintirorgon (LYC-55716), this agent selectively binds to the nuclear receptor transcription factor RORγ, forming a receptor complex that translocates to the nucleus, and binds to ROR response elements (ROREs), enhancing the function, proliferation and survival of type 17 T cells, including Th17 (helper T cells) and Tc17 (cytotoxic T cells). RORγ, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation, plays a key role in immune activation. Cintirorgon (LYC-55716) is also orally bioavailable, while the new generation of immuno-oncology drugs-ncluding PD-1/PD-L1 inhibitors are delivered by injection[1].

Clinical Trial
分子量

603.53

性状

Solid

Formula

C27H23F6NO6S

CAS 号

2055536-64-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 113.3 mg/mL(187.73 mM)

Ethanol : 100 mg/mL(165.69 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.6569 mL8.2846 mL16.5692 mL
5 mM0.3314 mL1.6569 mL3.3138 mL
10 mM0.1657 mL0.8285 mL1.6569 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

*以上所有助溶剂都可在本网站选购。