PD 123319 ditrifluoroacetate
(Synonyms: PD123319二(三氟乙酸盐),PD123319 ditrifluoroacetate;PD-123319 ditrifluoroacetate) 目录号 : GC17384A selective angiotensin II type 2 receptor antagonist
Cas No.:136676-91-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Description:
IC50 Value: 1.2 ±0.4 mM (Inhibition of adenylyl cyclase elicited by 0.1 microM Ang II) [2]
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.
in vitro: Neither the AT1 antagonist losartan nor the AT2 antagonist PD 123319 exhibited significant competition for [125I]angiotensin-(1-7) binding to endothelial cells isolated from bovine aorta, in agreement with the absence of detectable mRNAs encoding typical angiotensin receptor subtypes 1 or 2 (AT1 or AT2) [1]. In radioligand binding competition experiments, approximately 25% of the specific binding sites labeled by 125I-[Sar1]Ang II were inhibited by low concentrations of PD 123319 (0.1 to 10 nM), whereas the AT2 antagonist CGP 42112A was inactive at concentrations less than 0.1 microM [2].
in vivo: PD 123319 did not influence baseline CBF, but resulted in a minor BP decrease (10 control and 10 treated rats) [3]. Sixteen normal subjects aged 29.9+/-13.8 years (range 18-30 years) received an intravenous infusion of PD 123319 (10 mcg/minute for 5 minutes) and placebo, separated by one week. Haemodynamics (cardiac index, stroke index and systemic vascular resistance) were measured non-invasively using a BioZ.com thoracic impedance detection system. Blood pressure was measured from an arm cuff using oscillometry [4].
Toxicity: Losartan and PD-123319 each increased vascular renin distribution in both kidneys. Late losartan treatment had no effect on any of the parameters in either kidney, and PD-123319 had no effect on either kidney [5].
Clinical trial: N/A
Cas No. | 136676-91-0 | SDF | |
别名 | PD123319二(三氟乙酸盐),PD123319 ditrifluoroacetate;PD-123319 ditrifluoroacetate | ||
化学名 | (6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridine-6-carboxylic acid;2,2,2-trifluoroacetic acid;hydrate | ||
Canonical SMILES | CC1=C(C=CC(=C1)CN2C=NC3=C2CC(N(C3)C(=O)C(C4=CC=CC=C4)C5=CC=CC=C5)C(=O)O)N(C)C.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O | ||
分子式 | C35H34F6N4O7 | 分子量 | 736.66 |
溶解度 | ≥ 110.2 mg/mL in DMSO with ultrasonic and warming, ≥ 117.6 mg/mL in EtOH with gentle warming, ≥ 73.7 mg/mL in Water | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.3575 mL | 6.7874 mL | 13.5748 mL |
5 mM | 0.2715 mL | 1.3575 mL | 2.715 mL |
10 mM | 0.1357 mL | 0.6787 mL | 1.3575 mL |
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) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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,
体内配方配制方法:取 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 saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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