2. GPCR/G Protein
  3. CRFR
  4. Pexacerfont

Pexacerfont  (Synonyms: BMS-562086)

目录号: HY-12127 纯度: 99.97%
COA 产品使用指南

摩尔计算器

Pexacerfont 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂，作用于人 CRF1 受体，IC50 为 6.1±0.6 nM。

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Pexacerfont Chemical Structure

Pexacerfont Chemical Structure

CAS No. : 459856-18-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥500
In-stock
5 mg ￥1100
In-stock
10 mg ￥1600
In-stock
25 mg ￥3500
In-stock
50 mg ￥5600
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Pexacerfont 相关抗体

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CRFR1 CRFR2

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.

IC50 & Target

IC50: 6.1±0.6 nM (human CRF1 receptor)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
IMR-32 IC50
6.1 nM
Compound: 6, BMS-562086
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
[PMID: 21618986]
体外研究
(In Vitro)

Pexacerfont demonstrates a potent and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward human CRF1 receptor and has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors[1].

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

Pexacerfont 相关抗体:
体内研究
(In Vivo)

Pexacerfont (BMS-562086) is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus maze models of anxiety. After the intravenous bolus dose, the plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees. The CLp of Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). Assuming the value of CLp of Pexacerfont approximates the value of CLb in these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLp by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLb is equal to CLp is reasonable at least in rats, where the blood to plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose[1].

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

340.42

Formula

C18H24N6O
CAS 号
性状

固体

颜色

White to off-white

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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (146.88 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 2.9375 mL 14.6877 mL 29.3755 mL
5 mM 0.5875 mL 2.9375 mL 5.8751 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。-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。

  • 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 (7.34 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 (7.34 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 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。
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: 99.97%

COA (289 KB) HNMR (260 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Caco-2 cells at passage 50 to 60 are seeded on polycarbonate membranes of 24 well Transwell plates at a density of 60,000 cells/cm2. The cells are cultured for 21 to 25 days in culture medium consisting of Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum, 0.5 mM HEPES, 1% nonessential amino acids, 1% L-glutamine, 100 U/mL penicillin-G, and 100 μg/mL streptomycin. Before the permeability studies, apical (AP) and basolateral (BL) media are replaced with transport buffer (Hanks' balanced salt solution supplemented with 2% N, N-dimethylacetamide, pH 7.4). AP to BL permeability study is initiated by replacing the AP medium with the transport buffer containing 25 μM BMS-562086. All permeability experiments are performed at 37°C.Transepithelial electrical resistance (TEER) values are measured to assess cell monolayer integrity. TEER values are obtained both at the beginning and at the end of each experiment. Only wells with TEER values between 400 and 500 Ω/cm2 throughout the experiment are used in the studies. Mannitol (25 or 100 μM) transport experiments are performed in the same manner as other transport experiments. Mannitol served as a probe of the Caco-2 cell monolayer integrity[1].

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

Rats[1]
One group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with single jugular vein cannulas are designated for oral administration, and a second group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with dual jugular vein cannulas are designated for intravenous administration. All rats are fasted for approximately 18 h before use and for 4 h after dosing. Water is provided ad libitum. Pexacerfont (BMS-562086) is administered orally by gavage to three rats at a single dose of 5 mg/kg in 0.5% aqueous methylcellulose. A single intravenous bolus dose of Pexacerfont is administered to three rats at 1 mg/kg in 20% ethanol in saline via the jugular vein cannula. Blood samples (0.2 mL/time point per animal) are collected via the jugular vein cannula for analysis of Pexacerfont at 0, 0.08 (intravenous dose only), 0.17 (intravenous dose only), 0.25, 0.5, 0.75, 1, 2, 4, 8, 12, 24, 48, 72, and 96 h postdose. Plasma is prepared from the blood samples by centrifuging for 10 min at 1000g and 5°C.

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

Pexacerfont 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。-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
DMSO 1 mM 2.9375 mL 14.6877 mL 29.3755 mL 73.4387 mL
5 mM 0.5875 mL 2.9375 mL 5.8751 mL 14.6877 mL
10 mM 0.2938 mL 1.4688 mL 2.9375 mL 7.3439 mL
15 mM 0.1958 mL 0.9792 mL 1.9584 mL 4.8959 mL
20 mM 0.1469 mL 0.7344 mL 1.4688 mL 3.6719 mL
25 mM 0.1175 mL 0.5875 mL 1.1750 mL 2.9375 mL
30 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4480 mL
40 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8360 mL
50 mM 0.0588 mL 0.2938 mL 0.5875 mL 1.4688 mL
60 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL
80 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9180 mL
100 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7344 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:

Pexacerfont459856-18-9BMS-562086BMS562086BMS 562086CRFRCorticotropin-releasing Factor ReceptorCRHRInhibitorinhibitorinhibit

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