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PD 123319 ditrifluoroacetate Sale

(Synonyms: PD123319二(三氟乙酸盐),PD123319 ditrifluoroacetate;PD-123319 ditrifluoroacetate) 目录号 : GC17384

A selective angiotensin II type 2 receptor antagonist

PD 123319 ditrifluoroacetate Chemical Structure

Cas No.:136676-91-0

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5mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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

Chemical Properties

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
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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
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