PF-06372865 - 10mM in DMSO , CAS No.1614245-70-3

CAS: 1614245-70-3 Cat. No.: P655006 Formula: C₂₂H₂₁FN₄O₃S Molecular Weight: 440.49 PubChem CID: 76287260

GRADE & PURITY 10mM in DMSO

Storage

Protected from light,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA A receptors containing α1/α2/α3/α5 subunits ( K i s of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy

In Vitro

PF-06372865 (compound 34) has K i values of 0.18 nM, 2.9 nM, 1.1 nM, 18 nM for human GABA A α1β3γ2, α2β2γ2, α3β3γ2, α5β2γ2 and 0.34 nM, 4.58 nM for rat GABA A α1β3γ2, α2β2γ2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-06372865 (compound 34; 3, 10 mg/kg; orally; single dose) significantly increases the paw withdrawal threshold (PWT) in chronic constriction injury (CCI) animals . PF-06372865 (0.3, 3, 10 mg/kg for mouse and 1, 3, 10 mg/kg for rat; orally) exhibits efficacy in two models of epilepsy, PTZ induced seizures (mouse), and amygdala kindling (rat) . PF-06372865 (0.1, 0.32, 1, 3.2 and 10 mg/kg; orally) has anxiolytic activity at 3.2 and 10 mg/kg in elevated plus maze (male C57Bl/6 mice) . PF-06372865 has a T 1/2 of 1.1 hours, a Cl p of 22 mL/min/kg, and a V ss of 2.1 L/kg for rats . PF-06372865 has a T 1/2 of 0.9 hours, a Cl p of 29 mL/min/kg, and a V ss of 3.4 L/kg for dogs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Chronic constriction injury (CCI) model (male Wistar rats) Dosage: 3, 10 mg/kg Administration: Orally Result: Significantly increased paw withdrawal latency.

IC50& Target:Ki: 2.9 nM (α2), 21 nM (α1 PAM) and 134 nM (α2 PAM)

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA A receptors containing α1/α2/α3/α5 subunits ( K i s of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, resp

Storage

Protected from light,Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ACTIVATOR

Product Properties

• ALogP: 2.9

Names and Identifiers

• Isomeric SMILES: CCN1C=NC2=C1N=NC=C2C3=CC(=C(C=C3)F)C4=C(C=C(C=C4)S(=O)(=O)CC)OC
• Alternate CAS: 1614245-70-3
• PubChem CID: 76287260
• MeSH Entry Terms: 7-ethyl-4-(3-(4-ethylsulfonyl-2-methoxyphenyl)-4-fluorophenyl)imidazo(4,5-c)pyridazine;PF-06372865
• Molecular Weight: 440.49

Associated Targets(Human)

GABRA2 Tclin Gamma-aminobutyric acid receptor subunit alpha-2 (0 Activities)

Discover Target: GABRA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C, protected from light. The material is light-sensitive — keep it in its original opaque or amber container.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1614245-70-3, the molecular formula is C22H21FN4O3S, and the molecular weight is 440.49 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.