2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. RO1138452

RO1138452  (Synonyms: CAY10441)

目录号: HY-108912 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

RO1138452 是一种有效的选择性前列环素 IP (prostacyclin) 受体拮抗剂。RO1138452 对 IP 受体具有高的亲和力。在人血小板中，pKi 值为 9.3±0.1; 在重组 IP 受体系统中，pKi 值为 8.7±0.06。

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RO1138452 Chemical Structure

RO1138452 Chemical Structure

CAS No. : 221529-58-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1430
In-stock
1 mg ￥457
In-stock
5 mg ￥1300
In-stock
10 mg ￥2200
In-stock
25 mg ￥4600
In-stock
50 mg ￥7900
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

RO1138452 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.

IC50 & Target

Rat I2 Receptor

7 nM (IC50)

Rat I2 Receptor

8.33 (pKi)

Rabbit PAF Receptor

52.9 nM (IC50)

Human α2A adrenoceptor

724 nM (IC50)

Rat α1B adrenoceptor

3280 nM (IC50)

Human Muscarinic M4 Receptor

1450 nM (IC50)

Human muscarinic M2 Receptor

2220 nM (IC50)

Human muscarinic M1 Receptor

2570 nM (IC50)

Human muscarinic M5 Receptor

3110 nM (IC50)

Rat 5-HT1B Receptor

1130 nM (IC50)

pig 5-HT2C Receptor

1190 nM (IC50)

Rat 5-HT2A Receptor

3040 nM (IC50)

Human 5-HT1A Receptor

8580 nM (IC50)

Guinea-pig 5-HT4 Receptor

8910 nM (IC50)

Rat α1B adrenoceptor

5.87 (pKi)

Human α2A adrenoceptor

6.49 (pKi)

Human muscarinic M1 Receptor

5.66 (pKi)

Human muscarinic M5 Receptor

5.81 (pKi)

Human muscarinic M2 Receptor

5.88 (pKi)

Human muscarinic M4 Receptor

6.14 (pKi)

Rabbit PAF Receptor

7.9 (pKi)

Guinea-pig 5-HT4 Receptor

5.35 (pKi)

Human 5-HT1A Receptor

5.37 (pKi)

Rat 5-HT2A Receptor

5.71 (pKi)

Rat 5-HT1B Receptor

6.11 (pKi)

Pig 5-HT2C Receptor

6.11 (pKi)

体外研究
(In Vitro)

RO1138452 is IP receptor antagonist. The pIC50 values of RO1138452 in attenuating cAMP accumulation is 7.0±0.07. Functional antagonism of RO1138452 is studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor. The antagonist affinity (pKi) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme assays. RO1138452 displays affinity at imidazoline2 (I2) (8.3) and platelet activating factor (PAF) (7.9) receptors[1]. RO1138452 (10 pM-10 μM) added to cells concurrently with a fixed concentration of Taprostene (1 μM) prevents, in a concentration-dependent manner, the inhibition of CXCL9 and CXCL10 release, with p[A]50 (molar) values of -8.73±0.11 and -8.47±0.16 (p>0.05), respectively[2].

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

RO1138452 相关抗体:
体内研究
(In Vivo)

RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and anti-inflammatory potential. RO1138452 (1-10 mg/kg, i.v.) significantly reduces acetic acid-induced abdominal constrictions. RO1138452 (3-100 mg/kg, p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation. One hour after administration of RO1138452 (5 mg/kg, i.v.) to rats, the total plasma concentration is 0.189  μg/mL, whereas the free plasma concentrations is calculated to be 0.009 μg/mL (28 nM)[1].

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

309.41

Formula

C19H23N3O
CAS 号
性状

固体

颜色

Light yellow to brown

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (323.20 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)

Ethanol 中的溶解度 : 50 mg/mL (161.60 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2320 mL 16.1598 mL 32.3196 mL
5 mM 0.6464 mL 3.2320 mL 6.4639 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

In Vivo:

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 (8.08 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。

    以 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 (8.08 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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，请直接配置工作液。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： 50% PEG300    50% Saline

    Solubility: 10 mg/mL (32.32 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

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

COA (188 KB) HNMR (241 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

Selectivity is determined by the ability of RO1138452 (10 μM) to displace specific binding of standard radioligands at 51 receptors. When significant displacement of radioligand is observed (>70% for RO1138452), complete concentration-dependent displacement curves (in triplicate) are constructed to generate IC50 values. Displacement binding at the EP3 receptor is performed. Enzyme inhibition assays are also conducted. RO1138452 is evaluated at 10 μM in triplicate for inhibition of COX isoforms: COX-1 (ram seminal vesicle), COX-2 (sheep placenta and human umbilical vein). Arachidonic acid is used as a substrate and PGE2 accumulation is detected[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

BEAS-2B cells are incubated for 30 min at 37°C in supplement-free keratinocyte serum-free medium (KSFM) in the absence and presence of 100 nM RO1138452. Cells are washed with supplement-free KSFM, incubated in the same medium for defined periods, and exposed to 1 μM Taprostene. Four hours later, cells are harvested in reporter lysis buffer, and luciferase activity is measured. The viability HAECs and BEAS-2B cells is determined colorimetrically by measuring the reduction of the tetrazolium salt MTT to formazan, by mitochondrial dehydrogenases[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
Male Sprague-Dawley rats (n=3) are administered RO1138452 (5 mg/kg, i.v.). At various times after dose administration, the rats are anesthetized by halothane (5%), blood is collected by orbital bleed into a heparinized syringe and a plasma fraction is obtained by centrifugation of the blood at 2600× g for 5 min in a clinical centrifuge. The level of RO1138452 in each sample is determined by high-performance liquid chromatography with detection by mass spectrometry[1].

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

RO1138452 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.2320 mL 16.1598 mL 32.3196 mL 80.7989 mL
5 mM 0.6464 mL 3.2320 mL 6.4639 mL 16.1598 mL
10 mM 0.3232 mL 1.6160 mL 3.2320 mL 8.0799 mL
15 mM 0.2155 mL 1.0773 mL 2.1546 mL 5.3866 mL
20 mM 0.1616 mL 0.8080 mL 1.6160 mL 4.0399 mL
25 mM 0.1293 mL 0.6464 mL 1.2928 mL 3.2320 mL
30 mM 0.1077 mL 0.5387 mL 1.0773 mL 2.6933 mL
40 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0200 mL
50 mM 0.0646 mL 0.3232 mL 0.6464 mL 1.6160 mL
60 mM 0.0539 mL 0.2693 mL 0.5387 mL 1.3466 mL
80 mM 0.0404 mL 0.2020 mL 0.4040 mL 1.0100 mL
100 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8080 mL
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.

Keywords:

RO1138452221529-58-4CAY10441RO 1138452RO-1138452CAY 10441CAY-10441Prostaglandin ReceptorInhibitorinhibitorinhibit

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