1. Metabolic Enzyme/Protease
  2. MMP
  3. PD-166793

PD-166793 

Cat. No.: HY-107428
Handling Instructions

PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.

For research use only. We do not sell to patients.

PD-166793 Chemical Structure

PD-166793 Chemical Structure

CAS No. : 199850-67-4

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5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure[1][2][3].

IC50 & Target[1]

MMP-2

4 nM (IC50)

MMP-3

7 nM (IC50)

MMP-13

8 nM (IC50)

MMP-1

6.0 μM (IC50)

MMP-7

7.2 μM (IC50)

MMP-9

7.9 μM (IC50)

In Vitro

PD-166793 (0.1 μM) leads to a 20% inhibition of AMP deaminase (AMPD) activity in rat heart homogenates[2].
PD-166793 (100 μM; 36 h) significantly reduces MMP‐9 activity in normal human cardiac fibroblasts[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PD-166793 (1 mg/kg/d; daily gavage for 10 weeks) largely prevents the adverse remodeling characteristically seen in the aortocaval (AV) fistula model[3].
PD-166793 (5 mg/kg; oral gavage) exhibits superior pharmacokinetics (t1/2=43.6 h, Cmax=42.4 µg/mL, AUC0-∞=2822 µg•h/mL) in rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (6 weeks) were induced chronic biventricular volume overload[3]
Dosage: 1 mg/kg
Administration: Daily gavage beginning 2 weeks before surgery and continued until 8 weeks after surgery
Result: Prevented ventricular dilatation and attenuated the hypertrophy typically induced by chronic volume overload.
Molecular Weight

412.30

Formula

C₁₇H₁₈BrNO₄S

CAS No.

199850-67-4

SMILES

CC(C)[[email protected]@H](C(O)=O)NS(=O)(C1=CC=C(C2=CC=C(C=C2)Br)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PD-166793PD166793PD 166793MMPMatrix metalloproteinasesleftventricularremodelingdysfunctionprogressiveheartfailureInhibitorinhibitorinhibit

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PD-166793
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