L-371,257
目录号 : KM7896 CAS No. : 162042-44-6 纯度 : 98%

L-371,257 是一种口服生物有效的,不能透过血脑屏障的,竞争性的,选择性催产素受体 (oxytocin receptor) 拮抗剂 (pA2=8.4),对催产素受体 (Ki=19 nM) 和血管加压素 V1a 受体 (vasopressin V1a receptor,Ki=3.7 nM) 具有高亲和力。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).

IC50&Target

Ki: 19 nM (oxytocin receptor), 3.7 nM (vasopressin V1a receptor)

体内研究

Systemic administration of nonpenetrant oxytocin receptor antagonist L-371,257 (0.5 and 1.0 mg/kg; i.p. injection) stimulates weight gain in rats.

Animal Model: Six-hour fasted rats
Dosage: 0.5 and 1.0 mg/kg
Administration: Intraperitoneal injection (a single) 30-45 minutes prior to the start of the dark cycle and access to food; Intraperitoneal injection (given repeatedly) over 6 days.
Result: A single injection significantly stimulated weight gain at 0.5 and 1.0 mg/kg relative to vehicle treatment.
When given repeatedly over 6 days, 0.5 mg/kg significantly stimulated body weight gain (10.5±2.2 g) relative to vehicle treatment (4.7±2.7 g).
分子式
C28H33N3O6
分子量
507.58
CAS号
162042-44-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
暂无相关参考文献
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动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
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计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。