2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Naftidrofuryl oxalate

Naftidrofuryl oxalate  (Synonyms: Nafronyl oxalate salt)

製品番号: HY-B1107 純度: 99.94%
COA 取扱説明書 Technical Support

Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT2 receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT2 receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia.

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Naftidrofuryl oxalate

Naftidrofuryl oxalate 構造式

CAS 番号 : 3200-06-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 33 在庫あり
Solution
10 mM * 1 mL in DMSO USD 33 在庫あり
Solid
100 mg $30 在庫あり
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Naftidrofuryl oxalate 関連抗体

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製品説明

Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT2 receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT2 receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia[1][2][3].

IC50 & Target[1]

5-HT2 Receptor

 

体外実験

Naftidrofuryl (1 nM-10 μM) oxalate concentration-dependently protects human fibroblast and endothelial cells from hypoxic stress by increasing protein production and preserving ATP levels[2].
Naftidrofuryl (10 nM-1 mM) oxalate dose-dependently inhibits Serotonin-induced vasoconstriction in human saphenous vein and animal blood vessels[2].
Naftidrofuryl (1 μM) oxalate completely inhibits Serotonin-induced proliferation of vascular smooth muscle cells[2].
Naftidrofuryl (1-100 μM) oxalate inhibits Serotonin-stimulated inositol triphosphate synthesis[2].

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

Naftidrofuryl oxalate 関連抗体
体内実験

Naftidrofuryl (10-22.5 mg/kg) oxalate normalises metabolite levels and modulates glucose utilisation and energy transduction in rats exposed to intermittent hypoxia[2].
Naftidrofuryl (30 mg/kg/day; i.p.; daily; 1 to 3 months) oxalate attenuates age-related increases in vascular reactivity to serotonin in spontaneously hypertensive rats without altering heart rate or hypertension progression[2].
Naftidrofuryl (50 mg/kg/day; p.o.; daily; 12 weeks) oxalate attenuates PMN-related atherosclerotic lesion formation and preserves endothelial function in high cholesterol diet-fed rats[2].
Naftidrofuryl (1 mg/kg; i.v.; single dose) oxalate inhibits thrombus growth and reduces thrombus stability in hamster cheek pouch arterioles[2].
Naftidrofuryl (7 mg/kg; i.p.; twice daily; 8 weeks) oxalate mimics exercise training effects on skeletal muscle oxidative metabolism in old rats, with additive benefits when combined with training[2].
Naftidrofuryl (0.025-8 mg/kg; i.a. or i.m.; single dose) oxalate produces immediate, dose-dependent femoral artery vasodilation in dogs without altering arterial blood pressure[2].
Naftidrofuryl (50 mg/kg/day; p.o.; daily) oxalate prevents high cholesterol diet-induced platelet hyper-reactivity in rabbits without affecting normal platelet function[2].

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

Animal Model: Spontaneously Hypertensive Rats (SHR)[2]
Dosage: 30 mg/kg/day
Administration: i.p.; daily; 1 to 3 months
Result: Attenuated the age-related increase in vascular reactivity to serotonin.
Did not modify heart rate or the development of hypertension.
Animal Model: Rats (unstated specific strain)[2]
Dosage: 50 mg/kg/day
Administration: p.o.; daily; 12 weeks
Result: Caused focal rather than circumferential intimal proliferation.
Prevented hypercholesterolaemia-induced impairment of endothelial relaxation to acetylcholine in thoracic and abdominal aorta.
Normalised PMN-dependent generation of oxygen-centred free radicals.
Animal Model: Hamsters (unstated specific strain)[2]
Dosage: 1 mg/kg
Administration: i.v.; single dose
Result: Caused significant dose-related inhibition of thrombus growth that lasted for at least 2 hours.
Decreased thrombus stability as demonstrated by increased thrombus fragmentation.
Animal Model: Old rats (21 months old, unstated specific strain)[2]
Dosage: 7 mg/kg
Administration: i.p.; twice daily; 8 weeks
Result: Mimicked the effects of training on the oxidative metabolism of skeletal muscle.
Combining Naftidrofuryl treatment with exercise training resulted in additive beneficial effects.
Animal Model: Rabbits (unstated specific strain)[2]
Dosage: 50 mg/kg/day
Administration: p.o.; daily
Result: Prevented platelet hyper-reactivity in rabbits receiving a high cholesterol diet.
Had no effect on platelet functions in rabbits receiving a standard diet.
分子量

473.56

分子式

C26H35NO7
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(CC)CC)C(CC1=C2C=CC=CC2=CC=C1)CC3OCCC3.O=C(O)C(O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

DMSO : ≥ 100 mg/mL (211.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (211.17 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1117 mL 10.5583 mL 21.1166 mL
5 mM 0.4223 mL 2.1117 mL 4.2233 mL
10 mM 0.2112 mL 1.0558 mL 2.1117 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 (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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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体内:

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: ≥ 2.5 mg/mL (5.28 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.

    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: ≥ 2.5 mg/mL (5.28 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.

    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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (105.58 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
純度とドキュメンテーション

純度: 99.94%

COA (255 KB) HNMR (300 KB) RP-HPLC (248 KB) MS (229 KB)

取扱説明書 (2659 KB)
参考文献

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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.1117 mL 10.5583 mL 21.1166 mL 52.7916 mL
5 mM 0.4223 mL 2.1117 mL 4.2233 mL 10.5583 mL
10 mM 0.2112 mL 1.0558 mL 2.1117 mL 5.2792 mL
15 mM 0.1408 mL 0.7039 mL 1.4078 mL 3.5194 mL
20 mM 0.1056 mL 0.5279 mL 1.0558 mL 2.6396 mL
25 mM 0.0845 mL 0.4223 mL 0.8447 mL 2.1117 mL
30 mM 0.0704 mL 0.3519 mL 0.7039 mL 1.7597 mL
40 mM 0.0528 mL 0.2640 mL 0.5279 mL 1.3198 mL
50 mM 0.0422 mL 0.2112 mL 0.4223 mL 1.0558 mL
60 mM 0.0352 mL 0.1760 mL 0.3519 mL 0.8799 mL
80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6599 mL
100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5279 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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Naftidrofuryl oxalate Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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  • 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:

Naftidrofuryl3200-06-4Nafronyl5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorhuman saphenous veinhuman fibroblasts5-HT2 receptorscritical limb ischaemiahuman plateletsspontaneously hypertensive ratsendothelial cellsintermittent claudicationvascular smooth muscle cellsperipheral occlusive arterial diseaseInhibitorinhibitorinhibit

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