Vafidemstat (Synonyms: ORY-2001)

Name: Vafidemstat
Brand: MedChemExpress
SKU: HY-112623
Rating: 5.0 (2 reviews)

Art. -Nr.: HY-112623 Reinheit: 98.03% ee.: 99.68%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Vafidemstat Chemische Struktur

CAS. Nr. : 1357362-02-7

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
250 mg	Auf Lager	Estimated Time of Arrival: December 31
500 mg	Auf Lager	Estimated Time of Arrival: December 31
1 g	Auf Lager	Estimated Time of Arrival: December 31
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10 g	Angebot einholen

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This product is a controlled substance and not for sale in your territory.

Kundenbewertung

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Vafidemstat

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

MAO-A MAO-B

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor^[1].

IC₅₀ & Target

LSD1/MAO-B^[1]

In Vitro

Vafidemstat (ORY-2001), a dual LSD1/MAO-B inhibitor, is a novel epigenetic agent for the treatment of neurodegenerative diseases. LSD1 is a protein that participates in transcription regulation complexes; its modulation can be used to tweak transcriptional imbalances in neurodegenerative disease and redress neuroinflammation and cognitive deficit^[1]. Vafidemstat (ORY-2001) can be used in the treatment of Alzheimer's disease^[2].

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

Klinische Studie

Molekulargewicht

336.39

Formel

C₁₉H₂₀N₄O₂

CAS. Nr.

1357362-02-7

Appearance

Solid

Color

White to off-white

SMILES

NC1=NN=C(O1)CN[C@H]2[C@H](C3=CC=C(OCC4=CC=CC=C4)C=C3)C2

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (148.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9727 mL	14.8637 mL	29.7274 mL
5 mM	0.5945 mL	2.9727 mL	5.9455 mL
10 mM	0.2973 mL	1.4864 mL	2.9727 mL

View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: 5 mg/mL (14.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (14.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (14.86 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 98.03% ee.: 99.68%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (245 KB) HNMR (229 KB) NP-HPLC (880 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

Verweise

[1]. ORYZON presents data on the Phase I trial with ORY-2001 at the 13th International Conference on Alzheimer’s and Parkinson’s diseases

[2]. ORYZON Reports Financial Results and Corporate Update for the 1st Half Ended June 30, 2018.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9727 mL	14.8637 mL	29.7274 mL	74.3185 mL
	5 mM	0.5945 mL	2.9727 mL	5.9455 mL	14.8637 mL
	10 mM	0.2973 mL	1.4864 mL	2.9727 mL	7.4318 mL
	15 mM	0.1982 mL	0.9909 mL	1.9818 mL	4.9546 mL
	20 mM	0.1486 mL	0.7432 mL	1.4864 mL	3.7159 mL
	25 mM	0.1189 mL	0.5945 mL	1.1891 mL	2.9727 mL
	30 mM	0.0991 mL	0.4955 mL	0.9909 mL	2.4773 mL
	40 mM	0.0743 mL	0.3716 mL	0.7432 mL	1.8580 mL
	50 mM	0.0595 mL	0.2973 mL	0.5945 mL	1.4864 mL
	60 mM	0.0495 mL	0.2477 mL	0.4955 mL	1.2386 mL
	80 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9290 mL
	100 mM	0.0297 mL	0.1486 mL	0.2973 mL	0.7432 mL

Vafidemstat Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vafidemstat1357362-02-7ORY-2001ORY2001ORY 2001Histone DemethylaseMonoamine OxidaseMAOInhibitorinhibitorinhibit

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Vafidemstat (Synonyms: ORY-2001)

Kundenbewertung

Vafidemstat Related Antibodies

2 Publications Citing Use of MCE Vafidemstat

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen:

Alle Monoamine Oxidase Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Vafidemstat Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Vafidemstat Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report