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  2. GHSR
  3. Capromorelin Tartrate

Capromorelin Tartrate  (Synonyms: CP 424391-18)

目录号: HY-15243 纯度: 98.19%
COA 产品使用指南

Capromorelin Tartrate 是一种可口服的,有效的growth hormone secretagogue receptor (GHSR)激动剂,对hGHS-R1a的Ki值为 7 nM。

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Capromorelin Tartrate Chemical Structure

Capromorelin Tartrate Chemical Structure

CAS No. : 193273-69-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1010
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2 mg ¥500
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5 mg ¥700
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10 mg ¥1200
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25 mg ¥2600
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50 mg ¥4600
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100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of Capromorelin Tartrate:

查看 GHSR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.

IC50 & Target

Ki: 7 nM (hGHS-R1a)[2]

体外研究
(In Vitro)

Capromorelin stimulates GH release in rat pituitary cell cultures with EC50 of 3 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dogs receiving capromorelin (30 mg/mL) have food consumption that is significantly greater than dogs treated with placebo. All dogs in the capromorelin group gain weight by 0.52 kg, more than that of placebo group[1]. Capromorelin shows enhanced intestinal absorption in rodent models and exhibits superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%][2]. Capromorelin stimulates GH release in anesthesized rat model, with ED50 of 0.05 mg/kg iv[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

655.70

Formula

C32H41N5O10

CAS 号
性状

固体

颜色

White to off-white

中文名称

卡普瑞林酒石酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 100 mg/mL (152.51 mM; 超声助溶)

DMSO 中的溶解度 : 100 mg/mL (152.51 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5251 mL 7.6254 mL 15.2509 mL
5 mM 0.3050 mL 1.5251 mL 3.0502 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.81 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.81 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (76.25 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.19%

参考文献
Kinase Assay
[2]

Membranes are prepared from HEK293 cells (ATCC) stably transfected with the human GHS-R1a receptor cDNA in the plasmid pcDNA3.1neo. Competition radioligand binding assays are performed in 96-well format with GF/C filters pre-soaked in 0.3% polyethyleneimine. Assays are performed at room temperature for 1 h in duplicate using 50 pM [125I]-ghrelin and 1 μg membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2, 0.2% bovine serum albumin and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The membranes are harvested and washed three times with ice-cold ish buffer containing 50 mM HEPES, pH 7.4 and 10 mM MgCl2. IC50 and Ki values are determined using Prism by GraphpadTM. The Kd of [125I]-ghrelin at membranes expressing human GHS receptors is calculated to be 0.2 nM.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

The study tested capromorelin flavored oral solution with 30 mg/mL of capromorelin compared to a matched placebo flavored oral solution treatment (which contains all the ingredients of the formulation without capromorelin) administered for 4 days. Dogs are randomized into two groups, with Group 1 receiving placebo (0.1 mL/kg) and Group 2 receiving 3.0 mg/kg. Both groups are treated once a day at approximately 9 AM each day. The first day of dosing is considered Day 0. The placebo and test drug are administered by a syringe placed in the corner of the mouth. The Day 0 weight is used for dose calculations.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Capromorelin Tartrate 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.5251 mL 7.6254 mL 15.2509 mL 38.1272 mL
5 mM 0.3050 mL 1.5251 mL 3.0502 mL 7.6254 mL
10 mM 0.1525 mL 0.7625 mL 1.5251 mL 3.8127 mL
15 mM 0.1017 mL 0.5084 mL 1.0167 mL 2.5418 mL
20 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9064 mL
25 mM 0.0610 mL 0.3050 mL 0.6100 mL 1.5251 mL
30 mM 0.0508 mL 0.2542 mL 0.5084 mL 1.2709 mL
40 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.9532 mL
50 mM 0.0305 mL 0.1525 mL 0.3050 mL 0.7625 mL
60 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6355 mL
80 mM 0.0191 mL 0.0953 mL 0.1906 mL 0.4766 mL
100 mM 0.0153 mL 0.0763 mL 0.1525 mL 0.3813 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Capromorelin Tartrate
目录号:
HY-15243
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