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PD-166793

Catalog No. T20563 CAS 199850-67-4

Synonyms: PD-166793-0000, PD 166793, PD166793

PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3 and MMP-13.PD-166793 ameliorates myocardial ischemia and reperfusion injury in a rat model of heart failure.PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3, and MMP-13.

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PD-166793, CAS 199850-67-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 52.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 289.00
50 mg	In stock	$ 463.00
100 mg	In stock	$ 693.00
500 mg	In stock	$ 1,430.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 100%

Biological Description

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Description	PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3 and MMP-13.PD-166793 ameliorates myocardial ischemia and reperfusion injury in a rat model of heart failure.PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3, and MMP-13.
Targets&IC50	MMP9:7.9 μM, MMP1:6.0 μM, MMP13:8 nM, MMP7:7.2 μM, MMP3:7 nM, MMP2:4 nM
In vitro	In rat heart homogenates, PD-166793 at a concentration of 0.1 μM results in a 20% inhibition of AMP deaminase (AMPD) activity[2]. Additionally, when normal human cardiac fibroblasts are treated with PD-166793 at a concentration of 100 μM for 36 hours, there is a significant reduction in MMP‐9 activity[1].
In vivo	Administered at a dosage of 1 mg/kg per day through daily gavage for a duration of 10 weeks, PD-166793 largely prevents the adverse remodeling typically observed in the aortocaval (AV) fistula model[3]. Furthermore, in rats, PD-166793 administered at a dose of 5 mg/kg via oral gavage demonstrates superior pharmacokinetics, with a half-life (t1/2) of 43.6 hours, a maximum concentration (Cmax) of 42.4 µg/mL, and an area under the curve from 0 to infinity (AUC0-∞) of 2822 µg•h/mL[2].

Synonyms	PD-166793-0000, PD 166793, PD166793
Molecular Weight	412.3
Formula	C17H18BrNO4S
CAS No.	199850-67-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL(194.03 mM), Sonication is recommended.

References and Literature

1. Kaludercic N, et, al. Inhibiting metalloproteases with PD 166793 in heart failure: impact on cardiac remodeling and beyond. Cardiovasc Ther. Spring 2008;26(1):24-37. 2. O'Brien PM, et, al. Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors. J Med Chem. 2000 Jan 27;43(2):156-66. 3. Chancey AL, et, al. Effects of matrix metalloproteinase inhibition on ventricular remodeling due to volume overload. Circulation. 2002 Apr 23;105(16):1983-8.

Related compound libraries

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Inhibitor Library

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Keywords

PD-166793 199850-67-4 Proteases/Proteasome MMP PD-166793-0000 PD 166793 PD166793 inhibitor inhibit

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