[CAS NO. 1255517-78-2] Fanapanelhydrate

Name: Fanapanelhydrate
Brand: Arctom Scientific
SKU: AS949526

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PRODUCTS SPECIFICATIONS [1255517-78-2]

Distributor

Catalog

AS949526

Brand

Arctom Scientific

CAS

1255517-78-2

DESCRIPTION [1255517-78-2]

Overview

MDL	-
Molecular Weight	427.27
Molecular Formula	C14H17F3N3O7P
SMILES	O=C(N1CP(O)(O)=O)C(NC(C1=C2)=CC(C(F)(F)F)=C2N3CCOCC3)=O.[H]O[H]

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

Summary

Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

IC50 & Target

AMPA Receptor

In Vitro

In the cortical slice preparation assay, ZK200775 gave Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC50 values of 200 nM, 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ZK200775 elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD50 (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg i.v., whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9–26.5) mg/kg i.v., which affected motor coordination in the rotating rod, ED50 14.6 (12.1–17.6) mg/kg. ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats [1]. ZK200775 (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. ZK200775 showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00999284	Charite University, Berlin, Germany\|Bayer	Visual Acuity	December 1996	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL ( 11.70 mM ; Need ultrasonic)

H ₂ O : 5 mg/mL ( 11.70 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3404 mL	11.7022 mL	23.4044 mL
5 mM	0.4681 mL	2.3404 mL	4.6809 mL
10 mM	0.2340 mL	1.1702 mL	2.3404 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: ≥ 0.5 mg/mL (1.17 mM); Clear solution
2.

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

Solubility: ≥ 0.5 mg/mL (1.17 mM); Clear solution
3.

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

Solubility: ≥ 0.5 mg/mL (1.17 mM); Clear solution

* All of the co-solvents are available by MCE.