Art. -Nr.: HY-160955

Z218484536

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Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a K_d value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model.

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Reinheit: 97.65%
CAS. Nr.: 1223877-07-3
Formel: C₁₁H₁₀FN₅O
Molecular Weight:247.23

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Z218484536 Chemical Structure

CAS. Nr.: 1223877-07-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Z218484536 (40-2,000 nM, 24 h) inhibits the release of l-serine, with an IC₅₀ of 0.4 μM, and reduces cellular L-serine levels with an IC₅₀ of 0.38 μM in cultured astrocytes^[1].

Z218484536 (0.078-40 μM, 48 h) has no toxic effect on the proliferation of HepG2 cells^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_last	T_1/2	T_max	C_max	AUC_{INF_obs}	MRT_last	MRT_{INF_obs}
Mice	4 mg/kg	i.p.	1088.34 ng·h/mL	2.71 h	0.17 h	1420.54 ng/mL	1100.16 ng·h/mL	1.00 h	1.17 h

In Vivo

Z218484536 (0.5-20 mg/kg, i.p., once a day, 3 day) delays the onset of acute epilepsy, reduces the severity of seizures, and is anticonvulsant in a Pentylenetetrazole (PTZ) -induced acute epilepsy model^[1].

Z218484536 (2 mg/kg, 4 mg/kg, i.p., once a day 3 day) reduces hippocampal L-serine and D-serine levels in a Kainic acid (HY-N2309) (KA)-induced chronic TLE mouse model^[1].

Z218484536 (2 mg/kg, 4 mg/kg, i.p., once a day, 7 weeks) suppresses spontaneous seizures in TLE mice^[1].

Z218484536 (4 mg/kg, i.p., once a day, 7 day) not affect the mice's emotional state or motor ability^[1].

Z218484536 (1 mg/kg, 2 mg/kg, i.p.,2 weeks, once a day, 3.5 months) reduces epileptic activity in a cynomolgus monkey TLE model^[1].

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

Animal Model:

KA mouse model of chronic TLE^[1]
Dosage:

2 mg/kg, 4 mg/kg
Administration:

i.p., 7 weeks, once a day
Result:

Reduced SES frequency to 0.44 per day .
Not caused weight loss.

Animal Model:

PTZ-induced acute model of seizures^[1]
Dosage:

0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, 20 mg/kg
Administration:

i.p., 3 days, once a day
Result:

Delayed the onset of acute epilepsy .
The maximum anticonvulsant effect was observed at a concentration of 4 mg/kg

Chemical Information

CAS. Nr. 1223877-07-3
Appearance Solid
Molecular Weight 247.23
Formel C₁₁H₁₀FN₅O
Color White to off-white
SMILES

O=C(N/N=C/C1=CNN=C1C2=CC=C(F)C=C2)N
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (404.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0448 mL

20.2241 mL

40.4482 mL

5 mM

0.8090 mL

4.0448 mL

8.0896 mL

10 mM

0.4045 mL

2.0224 mL

4.0448 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sha L, et al. Pharmacological inhibition of PSPH reduces serine levels and epileptic seizures. Nat Chem Biol. 2025 Jun 2. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0448 mL	20.2241 mL	40.4482 mL	101.1204 mL
	5 mM	0.8090 mL	4.0448 mL	8.0896 mL	20.2241 mL
	10 mM	0.4045 mL	2.0224 mL	4.0448 mL	10.1120 mL
	15 mM	0.2697 mL	1.3483 mL	2.6965 mL	6.7414 mL
	20 mM	0.2022 mL	1.0112 mL	2.0224 mL	5.0560 mL
	25 mM	0.1618 mL	0.8090 mL	1.6179 mL	4.0448 mL
	30 mM	0.1348 mL	0.6741 mL	1.3483 mL	3.3707 mL
	40 mM	0.1011 mL	0.5056 mL	1.0112 mL	2.5280 mL
	50 mM	0.0809 mL	0.4045 mL	0.8090 mL	2.0224 mL
	60 mM	0.0674 mL	0.3371 mL	0.6741 mL	1.6853 mL
	80 mM	0.0506 mL	0.2528 mL	0.5056 mL	1.2640 mL
	100 mM	0.0404 mL	0.2022 mL	0.4045 mL	1.0112 mL

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Z218484536

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Z218484536 Related Classifications

HY-160955 Related Classifications