Balcinrenone AZD9977|cas:1850385-64-6|西域试剂

Balcinrenone AZD9977,99.85%

产品编号：Bellancom-120274| CAS NO：1850385-64-6| 分子式：C₂₀H₁₈FN₃O₅| 分子量：399.37

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货号	价格	库存与货期
Bellancom-120274	￥2500.00	杭州北京（现货）
Bellancom-120274	￥3900.00	杭州北京（现货）
Bellancom-120274	￥6900.00	杭州北京（现货）
Bellancom-120274	￥9900.00	杭州北京（现货）
Bellancom-120274	￥14800.00	杭州北京（现货）

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Balcinrenone AZD9977

产品介绍

Balcinrenone (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。Balcinrenone 用于心力衰竭和慢性肾病的研究。

生物活性

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

体外研究

Balcinrenone (AZD9977) and eplerenone activities on MR, GR, PR and AR in binding assays. The observed pK_i of MR, GR, and PR are 7.5, 5.4 and 4.6, respectively.
Functional interaction of Balcinrenone with MR is characterized in a reporter gene assay where the full-length MR drives a luciferase reporter gene in U2-OS cells. Balcinrenone antagonizes aldosterone-activated MR with an IC₅₀ of 0.28 μM. Whereas eplerenone is a full antagonist, Balcinrenone suppresses only 69% of the MR activity in this assay.
Species selective potencies of Balcinrenone 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.

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

体内研究

Balcinrenone (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. Balcinrenone is as efficacious as full MR antagonists on renal protection, despite the partial antagonism observed in in vitro assays.
Balcinrenone (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.

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

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.

体内研究

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

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.

性状

Solid

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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。