Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 8-10周 | ||
50 mg | ¥ 13,800 | 8-10周 | ||
100 mg | ¥ 17,500 | 8-10周 |
产品描述 | TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1]. |
体外活性 | TC-SP 14 (compound 14) neither inhibits nor induces human cytochrome P450 enzymes. TC-SP 14 is nonmutagenic and does not significantly inhibit the hERG channel [1]. |
体内活性 | TC-SP 14 (compound 14) (0-3 mg/kg, Orally, once) produces a dose-dependent reduction in circulating blood lymphocytes 24 h after dosing [1]. TC-SP 14 (0-3 mg/kg, Orally, daily for 10 days) significant reduces ovalbumin (OVA)-induced ear swelling [1]. TC-SP 14 (2-15 mg/kg, IV or PO, once) possesses acceptable characteristics [1]. Pharmacokinetic Parameters of TC-SP 14 in female Sprague-Dawley rats and male Cynomolgus [1]. species rat NHP CL (L/h/kg) 0.33 0.50 Vss (L/kg) 3.3 1.6 T 1/2 (h) 7.5 35.2 MRT (h) 10 3.3 % F 68 23 Animal Model: Lewis rats (female, n = 5/group) [1] Dosage: 0.3, 1.0, and 3.0 mg/kg Administration: Orally, once Result: Produced a dose-dependent reduction in circulating blood lymphocytes 24 h postdose, resulted in near maximal lymphopenia at 3.0 mg/kg (74% reduction in lymphocytes vs vehicle). Animal Model: OVA-immunized Lewis rats (female, n = 8/group) [1] Dosage: 0.1, 0.3, 1.0, and 3.0 mg/kg Administration: Orally, daily for 10 days Result: Significant reduced OVA-induced ear swelling at doses of 0.3 mg/kg and higher. Animal Model: Female Sprague-Dawley rats, Male Cynomolgus (NHP (nonhuman primates)) (n=3/group) [1] Dosage: 2 (IV, rat), 4 (IV, NHP), 10 (PO, NHP), 15 mg/kg (PO, rat) Administration: IV, PO, once (Pharmacokinetic Analysis) Result: Possessed acceptable characteristics, demonstrated low clearance, moderate steady state volumes of distribution, moderate-to-long mean residence times, and acceptable oral bioavailability. |
分子量 | 450.5 |
分子式 | C25H20F2N2O2S |
CAS No. | 1257093-40-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
TC-SP 14 1257093-40-5 TCSP 14 TC SP 14 Inhibitor inhibitor inhibit