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Product Introduction
Bioactivity
英文名: Etrasimod
描述: Etrasimod (APD334) 是一種特異性和口服的S1P1受體拮抗劑，在CHO 細(xì)胞中的IC50值為1.88 nM。
動(dòng)物實(shí)驗(yàn): APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose. APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose.
體外活性: 在表達(dá)HA標(biāo)記的S1P1的CHO細(xì)胞中，APD334的IC50值為1.88 nM。在人類S1P4和S1P5上觀察到中等程度的激動(dòng)作用，但與S1P1相比，無論是在效力還是效能方面均有所減少。APD334在人類S1P2和S1P3上沒有表現(xiàn)出任何激動(dòng)或拮抗作用。
體內(nèi)活性: APD334在所有物種中具有相對(duì)低的系統(tǒng)清除率（<4%的肝臟血流量）和高Cmax。在狗和猴子中，與嚙齒動(dòng)物相比觀察到分布體積（Vss）的顯著減少�？诜锢枚仍�40-100%范圍內(nèi)，末端半衰期在猴子中為6小時(shí)，而在狗中可長(zhǎng)達(dá)29小時(shí)。
存儲(chǔ)條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 25 mg/mL (54.64 mM)
關(guān)鍵字: LPL Receptor | Inhibitor | inhibit | APD-334 | Etrasimod | Lysophospholipid Receptor | APD 334
相關(guān)產(chǎn)品: Phorbol 12-myristate 13-acetate | SKI V | ML-031 | MP-A08 | K145 hydrochloride | LX-2931 | GLPG2938 | CYM5442 | ASP-4058 | SLP9101555
相關(guān)庫: Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Orally Active Compound Library | Bioactive Compound Library
Bioactivity
英文名: Etrasimod
描述: Etrasimod (APD334) 是一種特異性和口服的S1P1受體拮抗劑，在CHO 細(xì)胞中的IC50值為1.88 nM。
動(dòng)物實(shí)驗(yàn): APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose. APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose.
體外活性: 在表達(dá)HA標(biāo)記的S1P1的CHO細(xì)胞中，APD334的IC50值為1.88 nM。在人類S1P4和S1P5上觀察到中等程度的激動(dòng)作用，但與S1P1相比，無論是在效力還是效能方面均有所減少。APD334在人類S1P2和S1P3上沒有表現(xiàn)出任何激動(dòng)或拮抗作用。
體內(nèi)活性: APD334在所有物種中具有相對(duì)低的系統(tǒng)清除率（<4%的肝臟血流量）和高Cmax。在狗和猴子中，與嚙齒動(dòng)物相比觀察到分布體積（Vss）的顯著減少�？诜锢枚仍�40-100%范圍內(nèi)，末端半衰期在猴子中為6小時(shí)，而在狗中可長(zhǎng)達(dá)29小時(shí)。
存儲(chǔ)條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 25 mg/mL (54.64 mM)
關(guān)鍵字: LPL Receptor | Inhibitor | inhibit | APD-334 | Etrasimod | Lysophospholipid Receptor | APD 334
相關(guān)產(chǎn)品: Phorbol 12-myristate 13-acetate | SKI V | ML-031 | MP-A08 | K145 hydrochloride | LX-2931 | GLPG2938 | CYM5442 | ASP-4058 | SLP9101555
相關(guān)庫: Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Orally Active Compound Library | Bioactive Compound Library
手機(jī)版：Etrasimod
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