1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. PF-06372865

PF-06372865 

Cat. No.: HY-120874 Purity: 98.11%
Handling Instructions

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis 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.

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

PF-06372865 Chemical Structure

PF-06372865 Chemical Structure

CAS No. : 1614245-70-3

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Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
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5 mg USD 150 In-stock
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10 mg USD 250 In-stock
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25 mg USD 550 In-stock
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50 mg USD 850 In-stock
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100 mg USD 1350 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis 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[1].

IC50 & Target

Ki: 2.9 nM (α2), 21 nM (α1 PAM) and 134 nM (α2 PAM)[1]

In Vitro

PF-06372865 (compound 34) has Ki values of 0.18 nM, 2.9 nM, 1.1 nM, 18 nM for human GABAA α1β3γ2, α2β2γ2, α3β3γ2, α5β2γ2 and 0.34 nM, 4.58 nM for rat GABAA α1β3γ2, α2β2γ2[1].

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[1].
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)[1].
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)[1].
PF-06372865 has a T1/2 of 1.1 hours, a Clp of 22 mL/min/kg, and a Vss of 2.1 L/kg for rats[1].
PF-06372865 has a T1/2 of 0.9 hours, a Clp of 29 mL/min/kg, and a Vss of 3.4 L/kg for dogs[1].

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)[1]
Dosage: 3, 10 mg/kg
Administration: Orally
Result: Significantly increased paw withdrawal latency.
Clinical Trial
Molecular Weight

440.49

Formula

C₂₂H₂₁FN₄O₃S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (113.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2702 mL 11.3510 mL 22.7020 mL
5 mM 0.4540 mL 2.2702 mL 4.5404 mL
10 mM 0.2270 mL 1.1351 mL 2.2702 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.11%

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PF-06372865
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HY-120874
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