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PAM-2

Name: PAM-2
Brand: TargetMol
SKU: T219249
Rating: 4.5 (1 reviews)

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PAM-2 is a potent, orally active, blood-brain barrier-penetrant selective positive allosteric modulator of α7nAChR (human α7nAChREC50: 39 μM, rat α7nAChREC50: 12 μM), exhibiting anti-allodynic and anti-inflammatory properties. It shows selectivity for α9α10nAChR (IC50= 174 μM) and CaV2.2 channel (IC50= 89 μM). By enhancing α7nAChR activity, PAM-2 alleviates neuropathic pain induced by Streptozotocin (STZ) and Oxaliplatin in mice. PAM-2 is useful in the study of neuropathic pain.

Cas No. 1426293-61-9

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	PAM-2 is a potent, orally active, blood-brain barrier-penetrant selective positive allosteric modulator of α7nAChR (human α7nAChREC50: 39 μM, rat α7nAChREC50: 12 μM), exhibiting anti-allodynic and anti-inflammatory properties. It shows selectivity for α9α10nAChR (IC50= 174 μM) and CaV2.2 channel (IC50= 89 μM). By enhancing α7nAChR activity, PAM-2 alleviates neuropathic pain induced by Streptozotocin (STZ) and Oxaliplatin in mice. PAM-2 is useful in the study of neuropathic pain.
Targets & IC50	α7 nAChR (human):39 μM (EC50)
In vitro	PAM-2 (0.3 μM-1 mM; 5 minutes) enhances the activity of α7 nAChRs activated by acetylcholine (30 μM) in Xenopus oocytes in a concentration-dependent manner. Additionally, PAM-2 (0.3 μM-1 mM; 2 minutes) inhibits acetylcholine (10 μM)-induced currents via rα9α10 nAChRs in African clawed frog oocytes, showing concentration dependency but no voltage dependency. Moreover, PAM-2 (0.3 μM-1 mM) suppresses Ba2+ currents mediated by Ca v 2.2 channels in HEK293 cells, without affecting G protein-coupled GABA B R.
In vivo	PAM-2, administered orally at doses of 1 and 3 mg/kg on day 15 post-STZ, effectively alleviates neuropathic pain induced by STZ and Oxaliplatin in mice. Additionally, a 14-day co-administration of PAM-2 (1 mg/kg) with Oxaliplatin, followed by a single additional dose 30 minutes after the final co-administration, can prevent pain and increase the pain threshold.

Chemical Properties

Molecular Weight	227.26
Formula	C₁₄H₁₃NO₂
Cas No.	1426293-61-9
Smiles	N(C(/C=C/C1=CC=CO1)=O)C2=CC=C(C)C=C2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Related Tags: PAM-2 chemical structure | PAM-2 in vivo | PAM-2 in vitro | PAM-2 formula | PAM-2 molecular weight