| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
In rat cardiac homogenates, PD-166793 (0.1 μM) results in a 20% reduction of AMP deaminase (AMPD) activity [2]. In normal human cardiac fibroblasts, PD-166793 (100 μM; 36 hours) dramatically lowers MMP-9 activity [2].
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|---|---|
| ln Vivo |
PD-166793 (1 mg/kg/d; daily gavage for 10 weeks) largely prevents the typical adverse remodeling in aortoluminal (AV) fistula models [3]. PD-166793 (5 mg/kg; oral gavage) exhibits excellent pharmacokinetics in rats (t1/2=43.6 h, Cmax=42.4 µg/mL, AUC0-∞=2822 µg·h/mL )[1].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (6 weeks) were induced to chronic biventricular volume overload [3]
Doses: 1 mg/kg Route of Administration: Daily gavage starting 2 weeks before surgery and continuing until 8 weeks after surgery Weekly Experimental Results: Prevents ventricular dilation and attenuates hypertrophy commonly caused by chronic volume overload. |
| References |
|
| Molecular Formula |
C17H18BRNO4S
|
|---|---|
| Molecular Weight |
412.29
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| Exact Mass |
411.014
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| CAS # |
199850-67-4
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| PubChem CID |
9887870
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| Appearance |
White to pink solid powder
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| Density |
1.457g/cm3
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| Boiling Point |
562.069ºC at 760 mmHg
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| Melting Point |
192-193℃
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| Flash Point |
293.729ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
4.975
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
515
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)[C@@H](C(=O)O)NS(=O)(=O)C1=CC=C(C=C1)C2=CC=C(C=C2)Br
|
| InChi Key |
GJOCABIDMCKCEG-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C17H18BrNO4S/c1-11(2)16(17(20)21)19-24(22,23)15-9-5-13(6-10-15)12-3-7-14(18)8-4-12/h3-11,16,19H,1-2H3,(H,20,21)/t16-/m0/s1
|
| Chemical Name |
(2S)-2-[[4-(4-bromophenyl)phenyl]sulfonylamino]-3-methylbutanoic acid
|
| Synonyms |
PD166793; PD 166793; PD-166793
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~242.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4255 mL | 12.1274 mL | 24.2548 mL | |
| 5 mM | 0.4851 mL | 2.4255 mL | 4.8510 mL | |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4255 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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