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Ridaifen-B

CAS No. : 886465-70-9

MCE 站：Ridaifen-B

产品活性：Ridaifen-B (RID-B) 是一种有效的雌激素受体 (ERα) 拮抗剂，IC₅₀?值为 52.4 nM，是他莫西芬 (HY-13757A) 的衍生物。Ridaifen-B (RID-B) 是一种高亲和力，选择性，逆激动剂，作用于 CB₂ 受体 (K_i=43.7 nM)，是 CB₁ 受体 (K_i=300 nM) 选择性的 17 倍。Ridaifen-B 调节 G 蛋白 (IC₅₀=300 nM) 和腺苷基环化酶活性 (IC₅₀=134 nM)。Ridaifen-B 具有抗炎，抗肿瘤、抗破骨细胞的作用。Ridaifen-B 可诱导细胞凋亡和细胞自噬。

研究领域：Others  |  Neuronal Signaling  |  GPCR/G Protein  |  Autophagy  |  Apoptosis

作用靶点：Estrogen Receptor/ERR  |  Cannabinoid Receptor  |  Autophagy  |  Apoptosis

In Vitro: Ridaifen-B (0-4 μM; 4-24 hours) damages the Jurkat cells in a dose-dependent manner within 4 hours, the IC₅₀ rate is 4 μM. In a longer time, Ridaifen-B also injures Jurkat cells in a dose-dependent manner, similar to the previous results obtained with short-term (4-h), and the IC₅₀ rate is about 0.4 μM.
Ridaifen-B (0-4 μM; 4-24 hours) induces cell apoptosis, it activates Caspase-3 in a time-dependent manner, as well as cleaved pro-Caspase-3 to active caspase-3 in ER-negative Jurkat cells.
Ridaifen-B (300 nM-1 μM) co-incubates with LPS significantly decreases the E_max?of NO production to 19.4 μM, 22.0 μM, and 18.2 μM, respectively in RAW264.7 murine macrophages.
Ridaifen-B acts as an inverse agonist at CB₂?receptors for modulation of G-protein activity. The potency of RID-B to modulate G-protein activation is examined by employing a non-hydrolyzable radioactive analogue of GTP, [³⁵S]GTPγS, which hinds to G-proteins irreversibly when activated. The CB₂?agonist CP-55,940 increases G-protein activation with an EC₅₀ of 2.3 nM. However, RID-B decreases G-protein activation with an IC₅₀ of 300 nM.
Consistent with modulation of G-protein activity, RID-B increases adenylyl cyclase activity in a concentration-dependent manner, elevating cAMP levels with an I_max?of 398% and a potency (IC₅₀) of 134 nM.

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