Indapamide DEA controlled substance

别名: 吲达帕胺;N-(2-甲基-2,3-二氢-1H-吲哚基)- 3-氨磺酰基-4-氯-苯甲酰胺; 吲满胺; 吲满速尿;茚磺苯酰胺;吲哒帕胺;吲达帕安;(±)- 吲达帕胺标准品;吲达帕胺 EP标准品;吲达帕胺 USP标准品;吲达帕胺 标准品;吲达帕胺标准品(JP);吲达帕胺原药;N-(2-甲基-2,3-二氢-1H-吲哚基)-3-氨磺酰基-4-氯-苯甲酰胺
目录号: V11884 纯度: ≥98%
吲达帕胺(Natrilix、Noranat、Fludex、Tertensif)是一种强效噻嗪类利尿剂,用于治疗高血压和失代偿性心力衰竭。
Indapamide CAS号: 26807-65-8
产品类别: Potassium Channel
产品仅用于科学研究,不针对患者销售
规格 价格 库存 数量
10g
25g
50g
100g
Other Sizes

Other Forms of Indapamide:

  • (rac)-Indapamide-d3 (indapamide d3)
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InvivoChem产品被CNS等顶刊论文引用
产品描述
吲达帕胺(Natrilix、Noranat、Fludex、Tertensif)是一种强效噻嗪类利尿剂,用于治疗高血压和失代偿性心力衰竭。
生物活性&实验参考方法
体外研究 (In Vitro)
在离体灌注大鼠胰腺中,吲达帕胺(0.1-500 mg/L;20 分钟)降低了对葡萄糖输注的总胰岛素分泌反应[2]。吲达帕胺 (1-100 μM) 抑制骨吸收并促进成骨细胞生长 [3]。
体内研究 (In Vivo)
在自发性高血压大鼠 (SHR) 中,吲达帕胺(1 mg/kg/d;灌胃 8 周)可降低血压 [4]。接受 10 mg/kg/d 吲达帕胺的大鼠对氧化震颤素、去甲肾上腺素和酪胺的升压反应降低[1]。
动物实验
Animal/Disease Models: Male spontaneously hypertensive rats (11 weeks) [4]
Doses: 1 mg/kg
Route of Administration: Daily gavage for 8 weeks
Experimental Results: Blood pressure diminished by 16.9 mm Hg. Increased dp/dtmax, ejection fraction (EF) and fractional shortening (FS).
参考文献

[1]. Indapamide. Drugs 28, 189–235 (1984).

[2]. A further examination of the possible effects of indapamide on glucose tolerance and insulin secretion in the rat and mouse. J Pharm Pharmacol. 1981 Nov;33(11):735-7.

[3]. Indapamide, a thiazide-like diuretic, decreases bone resorption in vitro. J Bone Miner Res. 2001 Feb;16(2):361-70.

[4]. Indapamide lowers blood pressure by increasing production of epoxyeicosatrienoic acids in the kidney. Mol Pharmacol. 2013 Aug;84(2):286-95.

其他信息
Pharmacodynamics
Indapamide belongs to the sulfonamide diuretic class and is an effective antihypertensive drug that has been shown to prevent target organ damage. Administration of indapamide leads to water and electrolyte loss, with higher doses resulting in a stronger diuretic effect. Serious and clinically significant electrolyte disturbances can occur with indapamide use—for example, hypokalemia due to renal potassium loss can lead to QTc interval prolongation. Further electrolyte imbalances may occur due to renal excretion of sodium, chloride, and magnesium. Other changes caused by indapamide include elevated plasma renin and aldosterone levels, and decreased urinary calcium excretion. In many studies investigating the effects of indapamide on hypertensive patients with and without diabetes, glucose tolerance has not been significantly altered. However, further research is needed to assess the long-term metabolic effects of indapamide, as impaired glucose tolerance induced by thiazide derivatives may take several years to appear in non-diabetic patients.
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C16H16CLN3O3S
分子量
365.8345
精确质量
365.06
CAS号
26807-65-8
相关CAS号
(rac)-Indapamide-d3;1217052-38-4
PubChem CID
3702
外观&性状
White to off-white solid powder
密度
1.5±0.1 g/cm3
熔点
160-162°C
折射率
1.694
LogP
2.1
tPSA
100.88
氢键供体(HBD)数目
2
氢键受体(HBA)数目
5
可旋转键数目(RBC)
3
重原子数目
24
分子复杂度/Complexity
580
定义原子立体中心数目
0
InChi Key
NDDAHWYSQHTHNT-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H16ClN3O3S/c1-10-8-11-4-2-3-5-14(11)20(10)19-16(21)12-6-7-13(17)15(9-12)24(18,22)23/h2-7,9-10H,8H2,1H3,(H,19,21)(H2,18,22,23)
化学名
4-chloro-N-(2-methyl-2,3-dihydroindol-1-yl)-3-sulfamoylbenzamide
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
DMSO : ≥ 100 mg/mL (~273.35 mM)
H2O : ~0.67 mg/mL (~1.83 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (6.83 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。
*生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。

配方 2 中的溶解度: ≥ 2.5 mg/mL (6.83 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。
*20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (6.83 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。


请根据您的实验动物和给药方式选择适当的溶解配方/方案:
1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL;

3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果,工作液请现配现用!
6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 2.7335 mL 13.6676 mL 27.3351 mL
5 mM 0.5467 mL 2.7335 mL 5.4670 mL
10 mM 0.2734 mL 1.3668 mL 2.7335 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;

3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);

4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
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+
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计算结果:

工作液浓度 mg/mL;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Indapamide and Chlorthalidone to Reduce Urine Supersaturation for Kidney Stone Prevention
CTID: NCT06111885
Phase: Phase 2    Status: Recruiting
Date: 2024-10-30
Zilebesiran as Add-on Therapy in Patients With Hypertension Not Adequately Controlled by a Standard of Care Antihypertensive Medication (KARDIA-2)
CTID: NCT05103332
Phase: Phase 2    Status: Completed
Date: 2024-10-16
Treatment Optimisation for Blood Pressure With Single-Pill Combinations in India
CTID: NCT05683301
Phase: Phase 4    Status: Completed
Date: 2024-10-08
A Study to Evaluate the Efficacy and Safety of BR1015 Combination Therapy
CTID: NCT05878561
Phase: Phase 3    Status: Recruiting
Date: 2024-05-22
Evaluation of the Antihypertensive effectIveness, Tolerability, and Adherence With Amlodipine/ Indapamide/ Perindopril Triple Single-pill Combination in Hypertensive Patients Without Concomitant Antihypertensive Therapy (TRIPTYCH)
CTID: NCT06259175
Phase:    Status: Not yet recruiting
Date: 2024-04-17
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Efficacy and Safety Study of the Fixed-dose Combination of Olmesartan + Indapamide When Compared to the Isolated Drugs in the Treatment of Hypertension.
CTID: NCT05110898
Phase: Phase 3    Status: Unknown status
Date: 2
Fixed-Dose Combination of Perindopril/Amlodipine (Amlessa®) and Fixed-Dose Combination of Perindopril/Indapamide /Amlodipine (Co-Amlessa®) - Contribution to Management in newly diagnosed and uncontrolled hypertensive patients (PRECIOUS study)
CTID: null
Phase: Phase 3    Status: Completed
Date: 2017-11-30


Safety and efficacy of fixed dose combination of Indapamide SR 1.5 mg / Amlodipine versus Valsartan / Amlodipine over 12-week of treatment with conditional titration based on the blood pressure control, in patients with uncontrolled essential hypertension after 1 month of Amlodipine 5 mg run-in treatment. An international, randomized, double-blind, multicenter controlled study.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2013-08-22
Ensayo aleatorizado controlado sobre la terapia guiada por el antígeno carbohidrato 125 en los pacientes dados de alta por insuficiencia cardiaca aguda: efecto sobre la mortalidad a 1 año.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2011-08-02
Perindopril arginine/Amlodipine versus Valsartan/Amlodipine antihypertensive strategies: Efficacy and safety in mild to moderate hypertensive patients.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2010-11-24

生物数据图片
  • Expression of P450 enzymes in the kidney and urinary levels of 11,12- and 14,15-EETs, 11,12- and 14,15-DHETs, and 20-HETE measured using enzyme-linked immunosorbent assay (ELISA) kits. Kidneys and urine were collected from SHRs and WKY rats treated with saline, indapamide (IDP), or HCTZ. (A) mRNA levels of CYP2C23, CYP2J3, and CYP4A1 were determined by real-time polymerase chain reaction and normalized to GAPDH. N = 5; *P < 0.05 versus saline-treated WKYs; #P < 0.05 versus saline-treated SHRs. (B) Representative western blot depicting the protein expression of CYP2C23, sEH, CYP2J3, and CYP4A1. N = 3, duplicated three times. (C) 11,12-EET and 14,15-EET ratios. (D) 11,12-DHET and 14,15-DHET ratios. (E) EET:DHET ratios. (F) 20-HETE levels. N = 5; *P < 0.05 versus saline-treated WKYs; #P < 0.05 versus saline-treated SHRs.[4]. Indapamide lowers blood pressure by increasing production of epoxyeicosatrienoic acids in the kidney. Mol Pharmacol. 2013 Aug;84(2):286-95.
  • Levels of P450 enzymes and their metabolites in the renal microvessels. Renal microvessels were isolated from WKYs and SHRs treated with saline, indapamide (IDP), or HCTZ. (A and B) Representative western blots (A) and densitometry analyses (B) of CYP2C23, sEH, and CYP2J3. N = 3, duplicated three times; *P < 0.05 versus saline-treated WKYs; **,#P < 0.05 versus saline-treated SHRs. (C) 11,12-EET and 14,15-EET levels, 11,12-DHET and 14,15-DHET levels, and EET/DHET ratios were determined via an enzyme-linked immunosorbetn assay (ELISA) kit and normalized to the amount of protein in the tissues. N = 6; *P < 0.05 versus WKYs; #P < 0.05 versus saline-treated SHRs.[4]. Indapamide lowers blood pressure by increasing production of epoxyeicosatrienoic acids in the kidney. Mol Pharmacol. 2013 Aug;84(2):286-95.
  • Renal vascular cAMP levels and PKA expression in rats. Renal microvessels were isolated from SHRs and WKY rats treated with saline, indapamide (IDP), or HCTZ. (A) cAMP levels in renal microvessels were determined using the cAMP assay kit. N = 8; *P < 0.05 versus saline-treated WKYs; #P < 0.05 versus saline-treated SHRs. (B) Representative western blot and densitometry analysis for PKA. N = 3, duplicated three times; *P < 0.05 versus WKYs; #P < 0.05 versus saline-treated SHRs.[4]. Indapamide lowers blood pressure by increasing production of epoxyeicosatrienoic acids in the kidney. Mol Pharmacol. 2013 Aug;84(2):286-95.
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