溶解性 | DMSO 100 mg/mL Water 100 mg/mL Ethanol 100 mg/mL |
存贮条件 | 储存温度-20°C |
备注 | PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. |
生化机理 | Description:IC50 Value: 1.2 ±0.4 mM (Inhibition of adenylyl cyclase elicited by 0.1 microM Ang II) [2]PD 123319 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 |
别名 | 1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-;1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)- |
PD123319
PD123319 (订货以英文为准)
编号:P129377
CAS号:130663-39-7
分子式:C31H31N4O3-
分子量:507.60
产品名称 | PD123319 |
中文名称 | PD123319 |
CAS号 | 130663-39-7 |
分子式(M.F.) | C31H31N4O3- |
分子量(M.W.) | 507.60 |
储存条件 | -20°C储存 |
个人防护设备 | Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter |
RTECS | AC3600000 |
WGK德国 | 2 |
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