2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. RORγt inverse agonist 34

RORγt inverse agonist 34 (compound 5a) 是一种 RORγt 反向激动剂，它抑制 RORγt-LBD 的 IC50 为 0.094 μM。RORγt inverse agonist 34 用于银屑病研究。

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RORγt inverse agonist 34 Chemical Structure

RORγt inverse agonist 34 Chemical Structure

CAS No. : 2247604-77-7

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RORγt inverse agonist 34 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research[1].

IC50 & Target[1]

RORγt

0.094 μM (IC50)

体外研究
(In Vitro)

RORγt inverse agonist 34 影响 RORγt-LBD 对 SRC1 共激活肽的募集，IC50 为 0.094 μM[1]。
RORγt inverse agonist 34 有效抑制 Th17 细胞分化的 IC50 为 1.57 μM[1]。
RORγt inverse agonist 34 (1 μM, 1 h) 在小鼠肝微粒体中的半衰期为 18 min[1]。
RORγt inverse agonist 34 抑制 hERG 的 IC50 超过 40 μM, 表明对心脏毒性低[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RORγt inverse agonist 34 相关抗体:
体内研究
(In Vivo)

RORγt inverse agonist 34 (100 mg/kg, i.p., 每天, 7天) 在改善 Imiquimod (HY-B0180) 诱导的银屑病病变方面表现出显著效果[1]。
RORγt inverse agonist 34 (0.25% - 4% 软膏, 每天, 11 天)在 Imiquimod (HY-B0180) 诱导的银屑病小鼠模型中表现出抗银屑病效果[1]。
RORγt inverse agonist 34 (4% 软膏, 透皮给药, 用量约 50 g) 在 BALB/c 小鼠中，约 10min 在血浆中达到峰值，浓度为 0.075 μg/mL[1]。
RORγt inverse agonist 34 (10% - 20% mg/kg 软膏, 每天, 12 天) 在 BALB/c 鼠中无明显的急性毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The Imiquimod (HY-B0180) -induced psoriasis model was established with female BALB/c mice aged 8 to 10 weeks. A 2 cm × 3 cm area of hair on the backs of the mice was shaved using a depilatory cream to establish experimental areas. The shaved backs and right ears of the mice were treated with a daily topical dose of 62.5 mg of a commercially available 5% Imiquimod (HY-B0180) from day 1 to day 7. The mice in the normal group had a Vaseline Lanette cream applied as an alternative treatment[1].
Dosage: 100 mg/kg
Administration: i.p.,daily 7days
Result: Demonstrated notable anti-inflammatory properties in the mouse model of psoriasis, with the most prominent effects observed at a dose of 4%.
Demonstrated significant efficacy in mitigating the Lmiquimod (HY-B0180B) -induced abnormal spleen enlargement, which is comparable to the positive control Dexamethasone (HY-14648) by comparing the ratios of splenic weight to body weight among different groups of mice.
Exhibited more significant effects in alleviating ear inflammation compared to the positive control Dexamethasone (HY-14648) (5 mg/kg).
Inhibited the erythema and scaling for the back skinwas essentially comparable to that of Dexamethasone (HY-14648).
分子量

531.71

Formula

C31H37N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RORγt inverse agonist 34 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

RORγt inverse agonist 342247604-77-7RORγt inverse agonist34RORγt inverse agonist-34RORRAR-related orphan receptoranti-inflammatoryTh17 cellsimmunotherapypsoriasisInhibitorinhibitorinhibit

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目录号：
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