2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. 5-HT Receptor Dopamine Receptor MMP Potassium Channel
  4. PZ-1657 hydrochloride

PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder.

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

PZ-1657 hydrochloride

PZ-1657 hydrochloride Chemical Structure

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PZ-1657 hydrochloride Related Antibodies

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Description

PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder[1].

IC50 & Target[1]

5-HT7 Receptor

5 nM (Ki)

5-HT1A Receptor

292 nM (Ki)

5-HT2A Receptor

435 nM (Ki)

D2 Receptor

1004 nM (Ki)

5-HT6 Receptor

3282 nM (Ki)

MMP-9

 

Parmacokinetics
Species Dose Route Note AUC0-t MRT T1/2 Cmax Tmax F CL Vss
Rat[1] 10 mg/kg i.g. brain 14399 min·ng/mL 117.9 min 153.9 min 78.9 ng/mL 120 min / / /
Rat[1] 10 mg/kg i.g. plasma 55900 min·ng/mL 56.6 min 68.9 min 1056.7 ng/mL 15 min 57.2 % / /
Rat[1] 2 mg/kg i.v. brain 59513 min·ng/mL 89.9 min 137.4 min 527 ng/mL / / / /
Rat[1] 2 mg/kg i.v. plasma 19552 min·ng/mL 55.1 min / / / 100 % 84.6 mL/min/kg 10 L/kg
Molecular Weight

495.01

Formula

C23H28ClFN4O3S
SMILES

O=S(C1=CC=C(F)C=C1)(NC2CCN(CCOC3=CC=CC=C3C4=CN(C)N=C4)CC2)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PZ-1657 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PZ-1657PZ1657PZ 16575-HT ReceptorDopamine ReceptorMMPPotassium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorMatrix metalloproteinasesKcsAInhibitorinhibitorinhibit

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