A selective angiotensin II type 2 receptor antagonist
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PD 123319 (trifluoroacetate salt)

Item No. 16099

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S)-1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid, di(2,2,2-trifluoroacetate)
CAS Number
136676-91-0
Molecular Formula
C31H32N4O3 • 2CF3COOH
Formula Weight
736.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
O=C(O)[C@H]1N(C(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC4=C(N(CC5=CC=C(N(C)C)C(C)=C5)C=N4)C1.FC(F)(C(O)=O)F.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C31H32N4O3.2C2HF3O2/c1-21-16-22(14-15-26(21)33(2)3)18-34-20-32-25-19-35(28(31(37)38)17-27(25)34)30(36)29(23-10-6-4-7-11-23)24-12-8-5-9-13-24;2*3-2(4,5)1(6)7/h4-16,20,28-29H,17-19H2,1-3H3,(H,37,38);2*(H,6,7)/t28-;;/m0../s1
InChi Key
GPKQIEZLHVGJQH-ZXVJYWQYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $193

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    25 mg

    $424

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    50 mg

    $740

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    Product Description

    Angiotensin II is a peptide hormone that regulates blood pressure and fluid balance, contributing to hypertension, atherosclerosis, left ventricular hypertrophy, myocardial infarction, and heart failure. It binds with high affinity to two distinct receptors: AT1R (angiotensin type 1 receptor) and AT2R (angiotensin type 2 receptor). AT1R activation facilitates the ‘classical’ effects, including vasoconstriction, cellular growth, and proliferation, whereas AT2R activation offsets AT1R-mediated actions, promoting vasodilatation, apoptosis, and anti-growth effects.1 PD 123319 is a selective, nonpeptide AT2R antagonist (IC50 = 5.6 nM vs. 100 nM for AT1R).1,2 It has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bosnyak, S., Jones, E.S., Christopoulos, A., et al. Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin. Sci. (Lond.) 121(7), 297-303 (2011).

    2. Wexler, R.R., Greenlee, W.J., Irvin, J.D., et al. Nonpeptide angiotensin II receptor antagonists: The next generation in antihypertensive therapy. J. Med. Chem. 39(3), 625-656 (2014).

    3. Makino, N., Sugano, M., Otsuka, S., et al. Molecular mechanism of angiotensin II type I and type II receptors in cardiac hypertrophy of spontaneously hypertensive rats. Hypertension 30(4), 796-802 (1997).

    4. Daugherty, A., Rateri, D.L., Howatt, D.A., et al. PD123319 augments angiotensin II-induced abdominal aortic aneurysms through an AT2 receptor-independent mechanism. PLoS One 8(4), e61849 (2013).