CTAP

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CTAP

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

103429-32-9

CTAP 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 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 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 is a potent, highly selective, and BBB penetrantμopioid receptorantagonist, with anIC₅₀of 3.5 nM. CTAP displays over 1200-fold selectivity overδ opioid(IC₅₀=4500 nM) andsomatostatin receptors. CTAP 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)

体内研究
(In Vivo)

CTAP (0-1 mg/kg, IP, single) blocks morphine’s antinociceptive effect^[1].
CTAP (10 mg/kg; IP, single) has no effect on L-DOPA-induced limb, axial, orolingual, or locomotor abnormal involuntary movements^[1].
CTAP is stable in the blood and serum of rats (T_1/2>500 min), showing that the structure of this peptide offers enzymatic resistance^[2].
CTAP 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.

分子量

1104.30

Formula

C₅₁H₆₉N₁₃O₁₁S₂

CAS 号

103429-32-9

Sequence

{d-Phe}-Cys-Tyr-{d-Trp}-Arg-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7)

Sequence Shortening

{d-Phe}-CY-{d-Trp}-RT-{Pen}-T-NH2 (Disulfide bridge:Cys2-Pen7)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.