西博帕多 T5167
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 863513-91-1 | ¥7,130.00 | 询底价 |
1 mL | 863513-91-1 | ¥1,280.00 | 询底价 |
5 mg | 863513-91-1 | ¥1,160.00 | 询底价 |
2 mg | 863513-91-1 | ¥692.00 | 询底价 |
1 mg | 863513-91-1 | ¥473.00 | 询底价 |
50 mg | 863513-91-1 | ¥5,180.00 | 询底价 |
25 mg | 863513-91-1 | ¥3,460.00 | 询底价 |
10 mg | 863513-91-1 | ¥1,870.00 | 询底价 |
200 mg | 863513-91-1 | ¥9,630.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Cebranopadol
描述: Cebranopadol (GRT6005) 是镇痛 NOP 和阿片受体激动剂,对人 NOP、μ-阿片 (MOP)、κ-阿片 (KOP) 和 δ-阿片 (DOP) 受体的 Ki 值分别为 0.9、0.7、2.6 和 18 nM。
激酶实验: Rat MOP, KOP, and NOP receptor binding assays were run using membrane suspensions from rat brain without the cerebellum for MOP receptors; without the pons, medulla oblongata, and cerebellum for NOP receptors; and without the pons, medulla oblongata, cerebellum, and cortex for KOP receptors and the following tritium-labeled radioligands: [3H]DAMGO in the MOP receptor assay, [3H]nociceptin in the NOP receptor assay, and [3H]Ci-977 in the KOP receptor assay. The assay buffer used for the binding studies was 50 mM Tris-HCl (pH 7.4) supplemented with 0.05% sodium azide. The final assay volume of 250 μl/well included 2 nM [3H]DAMGO, 1 nM [3H]nociceptin, or 1 nM [3H]Ci-977 as a ligand in the MOP, NOP, or KOP receptor assays, respectively, and cebranopadol in dilution series. Cebranopadol was diluted with 25% DMSO in water to yield a final 0.5% DMSO concentration, which also served as a respective vehicle control. The assays were started by the addition of the membrane suspensions and, after short mixing, the assays were run for 90 minutes at room temperature. All incubations were run in triplicate and terminated by rapid filtration under mild vacuum and two washes of 5 ml of buffer using FP-100 Whatman GF/B filter mats. The radioactivity of the samples was counted after a stabilization and extraction period of at least 15 hours by use of the scintillation fluid Ready Protein; the complete competition curves for cebranopadol were recorded [1].
动物实验: The pharmacokinetic properties of cebranopadol in rats were investigated after a single intravenous dose of 160 μg/kg cebranopadol. The intravenous dose was administered as a bolus in a volume of 2 ml/kg with a catheter in the vena femoralis. Blood samples (200 μl/sample) were withdrawn via an implanted arterial catheter (arteria carotis) by an automated blood sampling system at the following sampling times: 0 (predose), 5, 15, 30, 60, 180, 360, 720, and 1440 minutes after administration. Blood samples were centrifuged, and plasma was separated. Plasma concentrations of cebranopadol were determined using a validated liquid chromatography-tandem mass spectrometry method. The lower limit of quantification for cebranopadol in this method was 0.05 ng/ml using a sample volume of 50 μl of plasma [1].
体外活性: Cebranopadol showed full agonistic efficacy at the human MOP and DOP receptors, almost full efficacy at the human NOP receptor, and partial efficacy at the human KOP receptor. In a functional [35S]GTPgS binding assay with membranes expressing the human 5-HT5A receptor, cebranopadol did not show agonistic or signirficant antagonistic effects at concentrations up to 10.0 μM [1].
体内活性: Cebranopadol exhibits highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain with ED50 values of 0.5-5.6 μg/kg after intravenous and 25.1 μg/kg after oral administration. Cebranopadol's duration of action is long (up to 7 hours after intravenous 12 μg/kg; >9 hours after oral 55 μg/kg in the rat tail-flick test) [1]. In streptozotocin (STZ)-treated rats, cebranopadol (i.pl.) reduced mechanical hypersensitivity in the ipsilateral paw but had no effect at the contralateral paw. In CCI rats, cebranopadol (i.pl.) showed antiallodynic activity at the ipsilateral paw. After administration to the contralateral paw, cebranopadol also showed ipsilateral antiallodynic activity, but with reduced potency and delayed onset. In diabetic mice, cebranopadol i.th. and i.c.v. decreased heat hyperalgesia with full efficacy and similar potency for both routes [2]. In NOP(-/-) mice morphine treatment produced the same signs of withdrawal as in NOP(+/+) animals, while cebranopadol treatment elicited a stronger withdrawal syndrome in NOP(-/-) than of NOP(+/+) mice [3].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 6 mg/mL
H2O : Insoluble
关键字: Inhibitor | inhibit | Opioid Receptor | GRT-6005 | Cebranopadol | GRT 6005
相关产品: (D-Ser2)-Leu-Enkephalin-Thr | Spinorphin | Nociceptin | BTRX-335140 | Endomorphin 2 TFA | Ac-RYYRWK-NH2 acetate | CP-866087 | Mianserin hydrochloride | ORL1 antagonist 1 | beta-Neoendorphin acetate(77739-21-0 free base)
相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compound Library
西博帕多 T5167信息由TargetMol中国为您提供,如您想了解更多关于西博帕多 T5167报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途