Ulimorelin

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Ulimorelin

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:

842131-33-3

TZP-101

Ulimorelin (TZP-101) 是生长素释放肽受体 (GRLN) 激动剂，EC₅₀为 29 nM，K_i为 16 nM。Ulimorelin 是一种促运动剂，通过竞争性拮抗α1-肾上腺素受体引起血管舒张。Ulimorelin 可以刺激肠蠕动，可用于营养不良。

生物活性

Ulimorelin (TZP-101) is aghrelin receptor (GRLN)agonist with anEC₅₀of 29 nM and aK_iof 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action atα1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition^[1]^[2]^[3].

体内研究
(In Vivo)

Ulimorelin (TZP-101; 0.3-5 mg/kg; i.v.) causes a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum^[1].
Ulimorelin (1, 3, 5 mg/kg; i.v.) causes a substantial and prolonged (~1 h) increase in colorectal propulsive activity and expulsion of colonic contents^[1].
Ulimorelin (p.o.; 8 mg/kg) has a C_maxof 0.39 μM and a AUC of 82 μMomin for rats. Ulimorelin (i.v.; 2 mg/kg) has a T_1/2of 50 mins, a CL of 24 mL/min/kg, and a V_ssof 1.7 L/kg for rats^[3].

Animal Model:	Male Sprague-Dawley rats^[1]
Dosage:	0.3, 1, 3, 5 mg/kg
Administration:	i.v.
Result:	Caused a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum.

Clinical Trial

分子量

538.65

Formula

C₃₀H₃₉FN₄O₄

CAS 号

842131-33-3

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.