Cat. No.: HY-B2082

Fursultiamine

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Fursultiamine is a vitamin B₁ derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B₁?deficiency, osteoarthritis (OA) and cancer research.

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Pureté: 99.71%
CAS No.: 804-30-8
Formule: C₁₇H₂₆N₄O₃S₂
Masse moléculaire:398.54

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fursultiamine Chemical Structure

CAS No.: 804-30-8

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Activité biologique
- Description
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Fursultiamine is a vitamin B₁ derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B₁?deficiency, osteoarthritis (OA) and cancer research^[1]^[2].

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform NF-κB :

In Vitro

Fursultiamine (10 μM, 24 h) inhibits Sorafenib (HY-10201)-induced cell death of HepG2 and Huh7, inhibits the cleavage of caspase-3 and PARP^[3], inhibits NF-κB signaling pathway.
Fursultiamine (100 μM, 12 h) inhibits LPS (HY-D1056)-induced expression of IL-6, IL-8 and MCP-1 in cell ARPE-19^[4].
Fursultiamine (100 μM, 12 h) enhances the mitochondrial respiration, reactivates mitochondrial pyruvate dehydrogenase, and improves the metabolic reprogramming under hypoxia conditions^[4].

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

Real Time qPCR^[4]

Cell Line:

ARPE-19
Concentration:

100 μM
Incubation Time:

12 h
Result:

Inhibited expression of IL-6, IL-8 and MCP-1.

In Vivo

Fursultiamine (100 mg/kg, ip for 8 weeks) reduces MMP-1 expression, exhibits chondroprotective efficacy in rabbit osteoarthritis models^[2].
Fursultiamine (50 mg/kg, po, once a day for 7 days) ameliorates laser induced choroidal neovascularization lesions (CNV) in mouse models^[4].

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

Animal Model:

rabbit osteoarthritis models^[2]
Dosage:

100 mg/kg
Administration:

ip for 8 weeks
Result:

Reduced osteoarthritis lesions.

Animal Model:

Laser-induced CNV lesion in mouse models^[4]
Dosage:

50 mg/kg
Administration:

po, once a day for 7 days
Result:

Ameliorated the CNV lesions.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 804-30-8
Appearance Solid
Masse moléculaire 398.54
Formule C₁₇H₂₆N₄O₃S₂
Color White to off-white
SMILES

O=CN(CC1=CN=C(C)N=C1N)/C(C)=C(SSCC2OCCC2)\CCO
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 106.7 mg/mL (267.73 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 6.67 mg/mL (16.74 mM)

* "≥" means soluble, but saturation unknown.

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

2.5092 mL

12.5458 mL

25.0916 mL

5 mM

0.5018 mL

2.5092 mL

5.0183 mL

10 mM

0.2509 mL

1.2546 mL

2.5092 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (6.27 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 (6.27 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 (6.27 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Instruction de manipulation (2659 KB)

Références

[1]. Fursultiamine alleviates choroidal neovascularization by suppressing inflammation and metabolic reprogramming

[2]. Kobayashi T, et al. Fursultiamine, a vitamin B1 derivative, enhances chondroprotective effects of glucosamine hydrochloride and chondroitin sulfate in rabbit experimental osteoarthritis. Inflamm Res. 2005 Jun;54(6):249-55. [Content Brief]

[3]. Xiao-Yi Xiong, et al. Toll-Like Receptor 4/MyD88-Mediated Signaling of Hepcidin Expression Causing Brain Iron Accumulation, Oxidative Injury, and Cognitive Impairment After Intracerebral Hemorrhage. Circulation. 2016 Oct 4;134(14):1025-1038. [Content Brief]

[4]. Wang J, et al., Hepcidin Downregulation Correlates With Disease Aggressiveness And Immune Infiltration in Liver Cancers. Front Oncol. 2021 Jun 30;11:714756. [Content Brief]

[5]. Do JY, et al., Fursultiamine Alleviates Choroidal Neovascularization by Suppressing Inflammation and Metabolic Reprogramming. Invest Ophthalmol Vis Sci. 2020 Oct 1;61(12):24. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.5092 mL	12.5458 mL	25.0916 mL	62.7290 mL
	5 mM	0.5018 mL	2.5092 mL	5.0183 mL	12.5458 mL
	10 mM	0.2509 mL	1.2546 mL	2.5092 mL	6.2729 mL
	15 mM	0.1673 mL	0.8364 mL	1.6728 mL	4.1819 mL
DMSO	20 mM	0.1255 mL	0.6273 mL	1.2546 mL	3.1364 mL
	25 mM	0.1004 mL	0.5018 mL	1.0037 mL	2.5092 mL
	30 mM	0.0836 mL	0.4182 mL	0.8364 mL	2.0910 mL
	40 mM	0.0627 mL	0.3136 mL	0.6273 mL	1.5682 mL
	50 mM	0.0502 mL	0.2509 mL	0.5018 mL	1.2546 mL
	60 mM	0.0418 mL	0.2091 mL	0.4182 mL	1.0455 mL
	80 mM	0.0314 mL	0.1568 mL	0.3136 mL	0.7841 mL
	100 mM	0.0251 mL	0.1255 mL	0.2509 mL	0.6273 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Fursultiamine

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

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Posttranslational Modification Library

FDA Kinase Inhibitor Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fursultiamine Related Classifications

HY-B2082 Related Classifications