Laropiprant (Synonyms: MK-0524)

目录号: HY-50175 纯度: 99.93%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Laropiprant 是一种有效的具有选择性的 DP 受体拮抗剂 (DP receptor)，K_i 值为 0.57 nM，对 TP 受体的 K_i 值为 2.95 nM。

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Laropiprant Chemical Structure

CAS No. : 571170-77-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1089	In-stock
1 mg	￥450	In-stock
5 mg	￥990	In-stock
10 mg	￥1500	In-stock
50 mg	￥4450	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Laropiprant:

Laropiprant sodium 询价

Laropiprant 相关产品

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DP EP FP IP TXA₂/TP TXB₂

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Laropiprant is a potent and selective DP receptor antagonist with K_i values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively^[1]^[2]^[3].

IC₅₀ & Target^[1]

0.57 nM (Ki)

TP Receptor

2.95 nM (Ki)

体外研究
(In Vitro)

Laropiprant (0.01-1000 μM; 10 mins; HEK293 cells) is an inverse agonist of DP1 cAMP signaling and reduces DP1 cAMP signaling below basal levels^[1].
Laropiprant (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression^[1].

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

体内研究
(In Vivo)

Laropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles^[3].

Pharmacokinetic Analysis in Male Sprague-Dawley rats^[3]

Route	Dose (mg/kg)	AUC_0-∞ (μM·hr)	Cl_p (mL/min/kg)	V_dss (L/kg)	T_1/2 (hr)
PO	1	22.7	1.9	0.7	7.4
PO	5	96.0	2.1	0.9	7.6
Route	Dose (mg/kg)	AUC_0-∞ (μM·hr)	C_max (μM)	T_max (hr)	F(%)
IV	5	52.6	15.6	1.2	/

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

Clinical Trial

分子量

435.90

Formula

C₂₁H₁₉ClFNO₄S

CAS 号

571170-77-9

性状

固体

颜色

White to off-white

中文名称

拉罗皮兰；各拉西酮

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

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (229.41 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2941 mL	11.4705 mL	22.9410 mL
5 mM	0.4588 mL	2.2941 mL	4.5882 mL
10 mM	0.2294 mL	1.1471 mL	2.2941 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 (5.74 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.74 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，此方案实验周期在半个月以上的动物实验酌情使用。
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玉米油中，混合均匀。

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

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: 99.93%

选择批次：

Data Sheet (631 KB) SDS (393 KB)

COA (296 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Labrecque P, et, al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767.

[2]. Sturino CF, et, al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806. [Content Brief]

[3]. Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33. [Content Brief]

Cell Assay ^[2]	Vena8Fluoro+ Biochips are coated with collagen (200 µg/mL) at 4°C overnight and thereafter blocked with bovine serum albumin (10 µg/mL) for 30 minutes at room temperature followed by washing steps. Whole blood collected in sodium citrate is incubated with 3, 3-dihexyloxacarbocyanine iodide (1 µM) in the dark for 10 minutes. PGD2 (30 nM), BW245c (3 nM) are added 10 min before the start of perfusion, and the DP antagonist BWA868c or Laropiprant (1 µM) are added 10 min before the agonists. In another set of experiments whole blood is treated with niacin (3 mM), acetylsalicylic acid (1 mM) or Laropiprant (1 µM and 10 µM) for 30 min. CaCl₂ at a final concentration of 1 mM is added 2 minutes before the perfusion over the collagen-coated chip. Perfusion is carried out at a shear rate of 30 dynes cm². Thrombus formation is recorded. Computerized image analysis is performed by DucoCell analysis software, where the area covered by the thrombus is calculated. Data are expressed as percent of area covered in a control sample^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Labrecque P, et, al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767. [2]. Sturino CF, et, al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806. [Content Brief] [3]. Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33. [Content Brief]

Cell Assay
^[2]

Vena8Fluoro+ Biochips are coated with collagen (200 µg/mL) at 4°C overnight and thereafter blocked with bovine serum albumin (10 µg/mL) for 30 minutes at room temperature followed by washing steps. Whole blood collected in sodium citrate is incubated with 3, 3-dihexyloxacarbocyanine iodide (1 µM) in the dark for 10 minutes. PGD2 (30 nM), BW245c (3 nM) are added 10 min before the start of perfusion, and the DP antagonist BWA868c or Laropiprant (1 µM) are added 10 min before the agonists. In another set of experiments whole blood is treated with niacin (3 mM), acetylsalicylic acid (1 mM) or Laropiprant (1 µM and 10 µM) for 30 min. CaCl₂ at a final concentration of 1 mM is added 2 minutes before the perfusion over the collagen-coated chip. Perfusion is carried out at a shear rate of 30 dynes cm². Thrombus formation is recorded. Computerized image analysis is performed by DucoCell analysis software, where the area covered by the thrombus is calculated. Data are expressed as percent of area covered in a control sample^[2].

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

参考文献

[1]. Labrecque P, et, al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767.

[2]. Sturino CF, et, al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806. [Content Brief]

[3]. Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33. [Content Brief]

Laropiprant 相关分类

Inflammation/Immunology Endocrinology

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2941 mL	11.4705 mL	22.9410 mL	57.3526 mL
	5 mM	0.4588 mL	2.2941 mL	4.5882 mL	11.4705 mL
	10 mM	0.2294 mL	1.1471 mL	2.2941 mL	5.7353 mL
	15 mM	0.1529 mL	0.7647 mL	1.5294 mL	3.8235 mL
	20 mM	0.1147 mL	0.5735 mL	1.1471 mL	2.8676 mL
	25 mM	0.0918 mL	0.4588 mL	0.9176 mL	2.2941 mL
	30 mM	0.0765 mL	0.3824 mL	0.7647 mL	1.9118 mL
	40 mM	0.0574 mL	0.2868 mL	0.5735 mL	1.4338 mL
	50 mM	0.0459 mL	0.2294 mL	0.4588 mL	1.1471 mL
	60 mM	0.0382 mL	0.1912 mL	0.3824 mL	0.9559 mL
	80 mM	0.0287 mL	0.1434 mL	0.2868 mL	0.7169 mL
	100 mM	0.0229 mL	0.1147 mL	0.2294 mL	0.5735 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:

Laropiprant571170-77-9MK-0524拉罗皮兰各拉西酮MK0524MK 0524Prostaglandin ReceptorDP receptorpharmacokineticsmetabolismacylglucuronideInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Laropiprant (Synonyms: MK-0524)

Customer Review

Other Forms of Laropiprant: