PNU-142633

Name: PNU-142633
Brand: TargetMol
SKU: T16556
Rating: 4.5 (1 reviews)

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Catalog No. T16556Cas No. 187665-65-2

PNU-142633 has anti-migraine efficacy. PNU-142633 is a high affinity and selective 5-HT1D receptor agonist (Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively).

PNU-142633

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Catalog No. T16556Cas No. 187665-65-2

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
10 mg	$1,170	35 days	35 days

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Product Introduction

Bioactivity

Description	PNU-142633 has anti-migraine efficacy. PNU-142633 is a high affinity and selective 5-HT1D receptor agonist (Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively).
Targets&IC50	5-HT1D receptor:6 nM （ki）
In vitro	Compared with 84% for that of Sumatriptan, in a cytosensor cell-based assay, the intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT [1].
In vivo	PNU-142633 fails to alter resistance in these vascular beds. PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation [1].

Chemical Properties

Molecular Weight	422.52
Formula	C₂₄H₃₀N₄O₃
Cas No.	187665-65-2
Smiles	CNC(=O)c1ccc2[C@H](CCN3CCN(CC3)c3ccc(cc3)C(N)=O)OCCc2c1
Relative Density.	no data available

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

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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