製品番号: HY-108610A

Edelfosine

Name: Edelfosine
Brand: MedChemExpress
SKU: HY-108610A
Price: 88.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(別名: ET-18-OCH3)

1 Cited Publications

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Edelfosine (ET-18-OCH3) is an orally active lipid raft modulator and apoptosis inducer that alters membrane fluidity and preferentially inserts into tumor cell membranes. Edelfosine recruits death receptor ligands (FasL/CD95L, TRAIL) and Bid to lipid rafts to form death-inducing signaling complexes, thereby initiating mitochondria-dependent apoptosis and inducing cytochrome c release. Edelfosine also exerts anti-inflammatory effects, promotes L-Selectin shedding, and causes no gastrointestinal or organ toxicity. In addition, Edelfosine inhibits nucleic acid and protein synthesis in Leishmania donovani and exhibits antiproliferative activity. Edelfosine can be used in research on multiple myeloma, inflammatory bowel diseases (such as ulcerative colitis and Crohn's disease), and visceral leishmaniasis.

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純度: 99.0%
CAS 番号: 70641-51-9
分子式: C₂₇H₅₈NO₆P
分子量:523.73

保管条件:

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

Edelfosine 構造式

CAS 番号: 70641-51-9

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化学情報
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Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	13.5 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line A431. Antiproliferative activity of compound was measured on human tumor cell line A431.	[PMID: 7707324]
A549	IC₅₀	3.5 μM Compound: 3, ET-18-OMe	Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA	[PMID: 23415083]
A549	IC₅₀	7.4 μM Compound: 3, ET-18-OMe	Cytotoxicity against human A549 cells by flow cytometric analysis Cytotoxicity against human A549 cells by flow cytometric analysis	[PMID: 23415083]
BXPC-3	IC₅₀	18.8 μM Compound: EDLF	Growth inhibition of human BxPC3 cells after 72 hrs by XTT assay Growth inhibition of human BxPC3 cells after 72 hrs by XTT assay	[PMID: 29547833]
CEM-SS	IC₅₀	4 μM Compound: ET-18-OMe	In vitro inhibition of CEM-SS cell growth by 50 % In vitro inhibition of CEM-SS cell growth by 50 %	[PMID: 2016713]
CEM-SS	IC₅₀	4 mM Compound: 10	Concentration of compound required to 50% growth inhibition of HIV-1 in CEM-SS cells Concentration of compound required to 50% growth inhibition of HIV-1 in CEM-SS cells	[PMID: 1901911]
FHC	IC₅₀	45 μM Compound: Edelfosine	In vitro inhibition of FHC normal human colon cell proliferation In vitro inhibition of FHC normal human colon cell proliferation	10.1016/S0960-894X(97)00433-2
HL-60	IC₅₀	1 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line HL-60. Antiproliferative activity of compound was measured on human tumor cell line HL-60.	[PMID: 7707324]
HL-60	IC₅₀	12 μM Compound: ET-18-oMe	Inhibition of Protein Kinase C (PKC) isolated from HL-60 human promyelocytic leukemia cells Inhibition of Protein Kinase C (PKC) isolated from HL-60 human promyelocytic leukemia cells	[PMID: 2342075]
HL-60	IC₅₀	2 μM Compound: Edelfosine	In vitro inhibition of HL-60 human promyelocytic leukemia cell proliferation In vitro inhibition of HL-60 human promyelocytic leukemia cell proliferation	10.1016/S0960-894X(97)00433-2
HL-60	IC₅₀	6.1 μM Compound: Edelfosine	Cytotoxicity measured in HL-60 leukemic cells after a 24 hr incubation period. Cytotoxicity measured in HL-60 leukemic cells after a 24 hr incubation period.	[PMID: 7707324]
HT-29	IC₅₀	2 μM Compound: Edelfosine	In vitro inhibition of the HT-29 transformed human colon cell proliferation In vitro inhibition of the HT-29 transformed human colon cell proliferation	10.1016/S0960-894X(97)00433-2
Jurkat	IC₅₀	12.2 μM Compound: Edelfosine	Cytotoxicity against human Jurkat cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay Cytotoxicity against human Jurkat cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay	[PMID: 21571403]
K562	IC₅₀	6.1 μM Compound: Edelfosine	Antiproliferative activity of compound was measured on human tumor cell line K-562. Antiproliferative activity of compound was measured on human tumor cell line K-562.	[PMID: 7707324]
MCF7	IC₅₀	9.3 μM Compound: 3, ET-18-OMe	Cytotoxicity against human MCF7 cells by flow cytometric analysis Cytotoxicity against human MCF7 cells by flow cytometric analysis	[PMID: 23415083]
MDA-MB-231	IC₅₀	5 μM Compound: Edelfosine	In vitro inhibition of estrogen receptor negative MDA-MB-231 human breast cancer cell proliferation In vitro inhibition of estrogen receptor negative MDA-MB-231 human breast cancer cell proliferation	10.1016/S0960-894X(97)00433-2
MDA-MB-435	IC₅₀	12 μM Compound: ET-18-OCH3	Cytotoxicity against human MDA-MB-435 cells after 3 days in serum free conditions by MTT assay Cytotoxicity against human MDA-MB-435 cells after 3 days in serum free conditions by MTT assay	[PMID: 16279790]
MDA-MB-435	IC₅₀	3 μM Compound: ET-18-OCH3	Inhibition of Akt phosphorylation in MDA-MB-435 cells after 2 hrs Inhibition of Akt phosphorylation in MDA-MB-435 cells after 2 hrs	[PMID: 16279790]
PANC-1	IC₅₀	25.7 μM Compound: EDLF	Growth inhibition of human PANC1 cells after 72 hrs by XTT assay Growth inhibition of human PANC1 cells after 72 hrs by XTT assay	[PMID: 29547833]
THP-1	CC₅₀	12.9 μM Compound: Edelfosine	Cytotoxicity against human THP-1 cells Cytotoxicity against human THP-1 cells	[PMID: 36944273]
THP-1	EC₅₀	1 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 24 hrs by propidium iodide staining based fluorescence microscopic analysis Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 24 hrs by propidium iodide staining based fluorescence microscopic analysis	[PMID: 29501944]
THP-1	IC₅₀	3.1 μM Compound: Edelfosine	Leishmanicidal activity against amastigote stage of Leishmania infantum expressing GFP infected in human THP1 cells after 48 hrs by flow cytometric analysis Leishmanicidal activity against amastigote stage of Leishmania infantum expressing GFP infected in human THP1 cells after 48 hrs by flow cytometric analysis	[PMID: 24448421]
THP-1	IC₅₀	4.9 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells after 24 hrs by propidium iodide staining-based flow cytometric analysis Cytotoxicity against human THP1 cells after 24 hrs by propidium iodide staining-based flow cytometric analysis	[PMID: 24448421]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay Cytotoxicity against human THP1 cells assessed as live cells in neubauer chamber after 24 hrs by trypan blue assay	[PMID: 21571403]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 24 hrs by propidium iodide staining based flow cytometry Cytotoxicity against human THP1 cells assessed as reduction in cell viability measured after 24 hrs by propidium iodide staining based flow cytometry	[PMID: 32223141]
THP-1	IC₅₀	4.96 μM Compound: Edelfosine	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs	[PMID: 32738977]

体外実験

Edelfosine (10 μM; 24-48 h) induces apoptosis in human multiple myeloma (MM) cell lines (MM144, MM1S, MM1R, RPMI-8226, OPM-2), leukemic Jurkat T lymphoid cells and JY B lymphoid cells, with MM144 cells showing the highest sensitivity; however, it does not induce apoptosis in Fas/CD95-deficient human OPM-2 MM cells^[1].
Edelfosine (10 μM; 15 h) induces the translocation of Fas/CD95, DR4, DR5, FADD, procaspase-8, activated caspase-8 and Bid to lipid rafts in human MM144 cells, thereby promoting the formation of the death-inducing signaling complex (DISC), which consists of Fas/CD95, FADD and caspase-8^[1].
Edelfosine (10 μM; 3-24 h) induces apoptosis in human MM144 cells, with this effect emerging after 15 h of incubation. Activation of caspase-3 and PARP is detectable at this time point, and over 50% of cell apoptosis is observed after 24 h of incubation^[1].
Edelfosine (5 μg/mL; 12 h, 18 h) delays spontaneous apoptosis of neutrophils compared with the medium-only control group^[2].
Edelfosine (0.01-5 μg/mL; 15 min) downregulates cell surface L-selectin, CD43 and CD44 (but not CD11a, CD11b or HLA) in a concentration-dependent manner, with an IC₅₀ of 0.29 μM for L-selectin downregulation^[2].
Edelfosine (1.9-95 μM; 4 h) inhibits Leishmania donovani amastigotes in J774A.1 macrophages. After 4 hours of treatment, its ED₅₀ value is 19.47 μM as detected by light microscopy and 23.16 μM as detected by flow cytometry^[3].

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

Apoptosis Analysis^[1]

Cell Line:

Human multiple myeloma (MM) cell lines (MM144, MM1S, MM1R, RPMI-8226, OPM-2)
Concentration:

10 μM
Incubation Time:

24 h, 48 h
Result:

Induced potent apoptotic responses in all tested MM cell lines. Showed higher sensitivity in MM144 cells (higher cell-surface Fas/CD95 content).
Produced similar apoptotic cell death rates in dexamethasone-sensitive MM1S cells and dexamethasone-resistant MM1R cells.

Immunofluorescence^[1]

Cell Line:

Human MM144 cells and primary MM cells from patients
Concentration:

10 μM
Incubation Time:

12 h
Result:

Potentiated coclustering of lipid rafts and Fas/CD95 in MM144 cells, as shown by yellow colocalization areas in merged confocal images.
Induced similar coclustering in primary MM cells from patients.

Western Blot Analysis^[1]

Cell Line:

Human MM144 cells
Concentration:

10 μM
Incubation Time:

15 h
Result:

Induced translocation of Fas/CD95, DR4, DR5, FADD, procaspase-8, cleaved active caspase-8 forms, and Bid into lipid raft fractions.
Achieved almost complete translocation of Fas/CD95, DR5, FADD, and Bid into lipid rafts.\n
Induced formation of DISC containing Fas/CD95, FADD, and caspase-8 in whole cell lysates and in isolated lipid raft fractions.
Had its induced DISC formation prevented by disruption of lipid rafts with methyl-β-cyclodextrin.

Apoptosis Analysis^[1]

Cell Line:

Fas/CD95-deficient human OPM-2 MM cells, and OPM-2 cells transduced with full-length Fas/CD95 or truncated FasΔ57C retrovirus
Concentration:

10 μM
Incubation Time:

24 h
Result:

Did not induce apoptosis in Fas/CD95-deficient OPM-2 cells. Restored sensitivity to edelfosine in OPM-2 cells transduced with full-length Fas/CD95.
Failed to restore sensitivity in OPM-2 cells transduced with truncated FasΔ57C.
Did not restore Fas/CD95 expression in Fas/CD95-deficient OPM-2 cells, nor increase Fas/CD95 expression in Fas/CD95-positive MM144 cells.

Apoptosis Analysis^[1]

Cell Line:

Human MM144 cells stably transfected with Bcl-Xₗ (MM144-Bcl-Xₗ) or empty vector (MM144-Neo)
Concentration:

10 μM
Incubation Time:

15 h (cytochrome c release); 24 h (apoptosis)
Result:

Induced apoptosis and cytochrome c release from mitochondria to the cytosol in MM144-Neo cells.
Had both induced cytochrome c release and apoptosis prevented by overexpression of Bcl-Xₗ.

体内実験

Edelfosine (2.5-5 mg/kg; p.o.; daily; 21 days) inhibits bentonite-induced paw edema in Swiss mice by 34% (2.5 mg/kg) and 49% (5 mg/kg), with no associated body weight loss^[2].
Edelfosine (5 mg/kg; p.o.; daily) reduces TNBS-induced ulcerative colitis severity in Wistar rats by 45.5% at 24 hours and 76.5% at 7 days post-TNBS administration, while abating neutrophil infiltration and supporting colon tissue repair^[2].
Edelfosine (40 mg/kg; p.o.; daily; up to 4 weeks) shows no cardiotoxicity, hepatotoxicity, renal toxicity, or gastrointestinal histologic damage in healthy Wistar rats, and does not inhibit colonic mucosal prostaglandin E₂ synthesis^[2].

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

Animal Model:

Swiss mice inflammation model^[2]
Dosage:

2.5 mg/kg; 5 mg/kg
Administration:

p.o.; daily; 21 days
Result:

Inhibited inflammation by 34%.\nInhibited inflammation by 49%.\nCaused no body weight loss during treatment.

Animal Model:

Wistar rats with Inflammatory bowel disease^[2]
Dosage:

5 mg/kg
Administration:

p.o.; daily
Result:

Protected against TNBS-induced body weight loss.\nReduced colon wet weight.\nInhibited colonic mucosal damage score by 45.5% at 24 hours post-TNBS administration.\nInhibited colonic mucosal damage score by 76.5% at 7 days post-TNBS administration.\nReduced ulcer formation, edema, and inflammatory cell infiltration in colon sections, with focal reparative processes observed.\nDramatically reduced colonic myeloperoxidase and neutrophil elastase activities.\nResulted in only submucosal focal mild inflammatory cell infiltration, compared to widespread intense infiltration in untreated controls.

Animal Model:

Healthy Wistar rats^[2]
Dosage:

40 mg/kg
Administration:

p.o.; daily; 1 week; 4 weeks
Result:

Caused no body weight loss or overt toxicity during 4 weeks of treatment.\nShowed no cardiotoxicity, hepatotoxicity, or renal toxicity via biochemical and functional analyses.\nCaused no histologic damage to kidney, liver, heart, or stomach tissue.\nDid not inhibit basal prostaglandin E2 synthesis in rat colonic mucosal samples (78 ± 10 pg PGE2/mg tissue in control vs. 83 ± 9 pg PGE2/mg tissue in treated rats).

化学情報

CAS 番号 70641-51-9
性状 Solid
分子量 523.73
分子式 C₂₇H₅₈NO₆P
Color White to off-white
SMILES

CCCCCCCCCCCCCCCCCCOCC(OC)COP([O-])(OCC[N+](C)(C)C)=O
別名

ET-18-OCH3
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (1)

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Sci Rep

Edelfosine induces cell cycle arrest and apoptosis in vascular smooth muscle cells to suppress neointimal hyperplasia. [Abstract]

2026 Mar 25. PMID: 41882161

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (47.73 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9094 mL

9.5469 mL

19.0938 mL

5 mM

0.3819 mL

1.9094 mL

3.8188 mL

10 mM

0.1909 mL

0.9547 mL

1.9094 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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体内:

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: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: 25 mg/mL (47.73 mM); Clear solution; Need ultrasonic

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:

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. Gajate C, et al. Edelfosine and perifosine induce selective apoptosis in multiple myeloma by recruitment of death receptors and downstream signaling molecules into lipid rafts. Blood. 2007;109(2):711-719. [Content Brief]

[2]. Mollinedo F, et al. Novel anti-inflammatory action of edelfosine lacking toxicity with protective effect in experimental colitis. J Pharmacol Exp Ther. 2009;329(2):439-449. [Content Brief]

[3]. Azzouz S, et al. Leishmanicidal activity of edelfosine, miltefosine and ilmofosine. Basic Clin Pharmacol Toxicol. 2005;96(1):60-65. [Content Brief]

[4]. Hac-Wydro K, et al. Effect of edelfosine on tumor and normal cells model membranes--a comparative study. Colloids Surf B Biointerfaces. 2010;76(1):366-369. [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, 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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9094 mL	9.5469 mL	19.0938 mL	47.7345 mL
	5 mM	0.3819 mL	1.9094 mL	3.8188 mL	9.5469 mL
	10 mM	0.1909 mL	0.9547 mL	1.9094 mL	4.7735 mL
	15 mM	0.1273 mL	0.6365 mL	1.2729 mL	3.1823 mL
	20 mM	0.0955 mL	0.4773 mL	0.9547 mL	2.3867 mL
	25 mM	0.0764 mL	0.3819 mL	0.7638 mL	1.9094 mL
	30 mM	0.0636 mL	0.3182 mL	0.6365 mL	1.5912 mL
	40 mM	0.0477 mL	0.2387 mL	0.4773 mL	1.1934 mL

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Edelfosine

1 Cited Publications

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Edelfosine

MedChemExpress（MCE）の使用を引用している文献 Edelfosine

Parasite アイソフォーム固有の製品をすべて表示

Bcl-2 Family アイソフォーム固有の製品をすべて表示

Cytochrome P450 アイソフォーム固有の製品をすべて表示

生物活性

製品説明

Cellular Effect

体外実験

体内実験

化学情報

Publications (1)

溶剤 & 溶解度

体外:

体内:

In Vivo Dissolution Calculator

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Keywords

最近チェックした製品

Edelfosine

MedChemExpress（MCE）の使用を引用している文献 Edelfosine

Parasite アイソフォーム固有の製品をすべて表示

Bcl-2 Family アイソフォーム固有の製品をすべて表示

Cytochrome P450 アイソフォーム固有の製品をすべて表示

生物活性

製品説明

Cellular Effect

体外実験

体内実験

化学情報

Publications (1)

溶剤 & 溶解度

体外:

体内:

In Vivo Dissolution Calculator

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Edelfosine 関連分類

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Keywords

最近チェックした製品