Art. -Nr.: HY-14920

Dexelvucitabine

(Synonyms: Reverset; d-d4FC)

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Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful agent against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.52%
CAS. Nr.: 134379-77-4
Formel: C₉H₁₀FN₃O₃
Molecular Weight:227.19

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Dexelvucitabine Chemical Structure

CAS. Nr.: 134379-77-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HIV-1

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
B16	IC₅₀	>200 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected B16 cell line In vitro inhibitory activity against growth of HIV infected B16 cell line	[PMID: 9873711]
CCRF-CEM	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against CEM cells Tested in vitro for anticancer activity against CEM cells	[PMID: 10072683]
CCRF-CEM	IC₅₀	100 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected CEM cell line In vitro inhibitory activity against growth of HIV infected CEM cell line	[PMID: 9873711]
CCRF-CEM	IC₅₀	127 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected CEM cells combined with murine CTLL-2T lymphoblast cell line In vitro inhibitory activity against growth of HIV infected CEM cells combined with murine CTLL-2T lymphoblast cell line	[PMID: 9873711]
DLD-1	IC₅₀	>200 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected DLD-1 cell line In vitro inhibitory activity against growth of HIV infected DLD-1 cell line	[PMID: 9873711]
HeLa	IC₅₀	>50 μM Compound: Beta-D-dd (table 3)	In vitro antiviral activity against HIV in HeLa CD4 cells In vitro antiviral activity against HIV in HeLa CD4 cells	10.1016/0960-894X(95)00472-6
HepG2	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against HepG2 cells Tested in vitro for anticancer activity against HepG2 cells	[PMID: 10072683]
HepG2	IC₅₀	>100 μM Compound: Beta-D-dd (table 3)	In vitro antiviral activity against HBV in Hep G2 cells In vitro antiviral activity against HBV in Hep G2 cells	10.1016/0960-894X(95)00472-6
HepG2	IC₅₀	>200 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected HepG2 cell line In vitro inhibitory activity against growth of HIV infected HepG2 cell line	[PMID: 9873711]
LNCaP	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against LNCaP cells Tested in vitro for anticancer activity against LNCaP cells	[PMID: 10072683]
MCF7	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against MCF-7 cells Tested in vitro for anticancer activity against MCF-7 cells	[PMID: 10072683]
MT2	IC₅₀	100 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected MT-2/IIIB cell line In vitro inhibitory activity against growth of HIV infected MT-2/IIIB cell line	[PMID: 9873711]
PC-3	IC₅₀	>10 μM Compound: 6a	Tested in vitro for anticancer activity against PC-3 cells Tested in vitro for anticancer activity against PC-3 cells	[PMID: 10072683]
Rat1	IC₅₀	>200 μM Compound: ent-1	In vitro inhibitory activity against growth of HIV infected Rat-1 cell line In vitro inhibitory activity against growth of HIV infected Rat-1 cell line	[PMID: 9873711]
SK-MEL-28	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against SK-MEL-28 cells Tested in vitro for anticancer activity against SK-MEL-28 cells	[PMID: 10072683]
SK-MES-1	IC₅₀	>100 μM Compound: 6a	Tested in vitro for anticancer activity against SK-MES-1 cells Tested in vitro for anticancer activity against SK-MES-1 cells	[PMID: 10072683]
Vero	IC₅₀	>100 μM Compound: 6a	Tested in vitro for cytotoxicity against Vero cells Tested in vitro for cytotoxicity against Vero cells	[PMID: 10072683]

In Vivo

Dexelvucitabine (Reverset; d-d4FC; 33.3 mg/kg by i.v. or p.o.) has distribution and elimination half-lives (t_1/2α and t_1/2β, respectively) of 0.7 and 3.6 h in monkeys, respectively. The C_max ranges from 21.1 to 47.5 μM^[2].
Dexelvucitabine has a favorable pharmacokinetic profile with a long half-life (4.71 and 10.75 h after administration by the intravenous [i.v.] and oral [p.o.] routes, respectively) in woodchucks^[2].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 134379-77-4
Appearance Solid
Molecular Weight 227.19
Formel C₉H₁₀FN₃O₃
Color White to off-white
SMILES

O=C1N(C=C(C(N)=N1)F)[C@]2([H])O[C@@H](C=C2)CO
Synonyms

Reverset; d-d4FC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (220.08 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

4.4016 mL

22.0080 mL

44.0160 mL

5 mM

0.8803 mL

4.4016 mL

8.8032 mL

10 mM

0.4402 mL

2.2008 mL

4.4016 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.

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 (11.00 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 (11.00 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 (11.00 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 (273 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]. Brenda I Hernandez-Santiago, et al. Antiviral and cellular metabolism interactions between Dexelvucitabine and lamivudine. Antimicrob Agents Chemother. 2007 Jun;51(6):2130-5. [Content Brief]

[2]. L Ma, et al. Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys. Antimicrob Agents Chemother. 1999 Feb;43(2):381-4. [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	4.4016 mL	22.0080 mL	44.0160 mL	110.0401 mL
	5 mM	0.8803 mL	4.4016 mL	8.8032 mL	22.0080 mL
	10 mM	0.4402 mL	2.2008 mL	4.4016 mL	11.0040 mL
	15 mM	0.2934 mL	1.4672 mL	2.9344 mL	7.3360 mL
	20 mM	0.2201 mL	1.1004 mL	2.2008 mL	5.5020 mL
	25 mM	0.1761 mL	0.8803 mL	1.7606 mL	4.4016 mL
	30 mM	0.1467 mL	0.7336 mL	1.4672 mL	3.6680 mL
	40 mM	0.1100 mL	0.5502 mL	1.1004 mL	2.7510 mL
	50 mM	0.0880 mL	0.4402 mL	0.8803 mL	2.2008 mL
	60 mM	0.0734 mL	0.3668 mL	0.7336 mL	1.8340 mL
	80 mM	0.0550 mL	0.2751 mL	0.5502 mL	1.3755 mL
	100 mM	0.0440 mL	0.2201 mL	0.4402 mL	1.1004 mL

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Dexelvucitabine

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Human Metabolite Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dexelvucitabine

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Human Metabolite Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dexelvucitabine Related Classifications

HY-14920 Related Classifications