CTAP TFA 是一种强效、高选择性的、可透过血脑屏障的阿片受体 (μ opioid receptor) 拮抗剂，IC50为 3.5 nM。CTAP TFA 对δ opioid受体 (IC50=4500 nM) 和生长抑素受体 (somatostatin receptors) 具有超过 1200 倍的选择性。CTAP TFA 可用于L -多巴胺 (HY-N0304) 诱导的运动障碍 (LID) 和阿片类药物过量或成瘾的研究。
| 生物活性 | CTAP TFA is a potent, highly selective, and BBB penetrantμopioid receptorantagonist, with anIC50of 3.5 nM. CTAP TFA displays over 1200-fold selectivity overδ opioid(IC50=4500 nM) andsomatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction[1][2]. |
| IC50& Target | μ Opioid Receptor/MOR 3.5 nM (IC50) | δ Opioid Receptor/DOR 4500 nM (IC50) |
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体内研究
(In Vivo) | CTAP TFA (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect[1].
CTAP TFA (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements[1].
CTAP TFA is stable in the blood and serum of rats (T1/2>500 min), showing that the structure of this peptide offers enzymatic resistance[2].
CTAP TFA is extensively protein-bound to albumin in the perfusion medium (68.2%) and to proteins in rat serum (84.2%)[2].
| Animal Model: | Male Sprague-Dawley rats[1] | | Dosage: | 0, 0.1, 0.5, 1 mg/kg | | Administration: | IP, single | | Result: | Completely blocked morphine’s antinociceptive effect at 0.5 or 1 mg/kg. |
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| 分子量 | |
| 性状 | |
| Formula | |
| Sequence | Phe-Cys-Tyr-Trp-Arg-Thr-Pen-Thr-NH2 (Disulfide bridge:Cys2-Pen7) |
| Sequence Shortening | FCYWRT{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7) |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture and light, under nitrogen | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(82.08 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.8208 mL | 4.1040 mL | 8.2080 mL | | 5 mM | 0.1642 mL | 0.8208 mL | 1.6416 mL | | 10 mM | 0.0821 mL | 0.4104 mL | 0.8208 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 (sealed storage, away from moisture and light, under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
