AZD9977
目录号 : KM10297 CAS No. : 1850385-64-6 纯度 : 98%

AZD9977 是一种有效的,选择性的,具有口服活性的盐皮质激素受体 (MR) 调节剂。AZD9977 用于心力衰竭和慢性肾病的研究。

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

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生物活性

AZD9977 is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. AZD9977 is used for heart failure, and chronic kidney disease research.

体外研究

AZD9977 and eplerenone activities on MR, GR, PR and AR in binding assays. The observed pKi of MR, GR, and PR are 7.5, 5.4 and 4.6, respectively.
Functional interaction of AZD9977 with MR is characterized in a reporter gene assay where the full-length MR drives a luciferase reporter gene in U2-OS cells. AZD9977 antagonizes aldosterone-activated MR with an IC50 of 0.28 μM. Whereas eplerenone is a full antagonist, AZD9977 suppresses only 69% of the MR activity in this assay.
Species selective potencies of AZD9977 are established in reporter gene assays using the MR LBDs from human, mouse or rat. The corresponding IC50 values are 0.37 μM, 0.08 μM and 0.08μM, respectively.

体内研究

AZD9977 (oral administration; 10-100 mg/kg; 4 weeks) dose dependently reduces the UACR compared to vehicle in uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet. AZD9977 is as efficacious as full MR antagonists on renal protection, despite the partial antagonism observed in in vitro assays.
AZD9977 (oral administration; 100 mg/kg; co-administration with enalapril) stops further disease progression and reduces the urine albumin excretion (UAE) compared to vehicle treatment. Co-administration of enalapril has an apparent additive effect on UAE reduction, although this reduction is not statistically significant.

Animal Model: Uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet with AZD9977
Dosage: 10, 30 and 100 mg/kg
Administration: Oral administration; 10-100 mg/kg; 4 weeks
Result: Improved kidney function and histology in animal models of CKD.
Animal Model: Db/db mice uni-nephrectomised at 8 weeks of age are treated from age 18w to age 22w
Dosage: 100 mg/kg
Administration: Oral administration; 100 mg/kg; co-administration with enalapril
Result: Reduced albuminuria in diabetic kidney disease.
Co-administration of enalapril with AZD9977 had an additive effect on renal pathology scoring.
分子式
C20H18FN3O5
分子量
399.37
CAS号
1850385-64-6
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
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (625.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5039 mL 12.5197 mL 25.0394 mL
5 mM 0.5008 mL 2.5039 mL 5.0079 mL
10 mM 0.2504 mL 1.2520 mL 2.5039 mL
*

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。

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

  • 1.

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

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.21 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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