Referencia número: HY-17427

Emtricitabine

(Synonyms: BW1592)

8 Cited Publications

Revisión del cliente

Based on 8 publication(s) in Google Scholar

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC₅₀ of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.97%
No. CAS: 143491-57-0
Fòrmula: C₈H₁₀FN₃O₃S
Peso molecular:247.25

Almacenamiento:

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

Emtricitabine Chemical Structure

No. CAS: 143491-57-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (8)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC₅₀ of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.

IC₅₀ & Target

HIV-1

HIV-2

Ver todos los productos específicos de isoformas HIV :

Ver todos los productos específicos de isoformas Endogenous Metabolite :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	>100 μM Compound: 1d; FTC	Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days	[PMID: 32515595]
CCRF-CEM	CC₅₀	>100 μM Compound: 3; (-)-FTC	Cytotoxicity against human CEM cells measured after 6 days Cytotoxicity against human CEM cells measured after 6 days	[PMID: 37393791]
CCRF-CEM	EC₅₀	0.04 μM Compound: FTC	Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days	[PMID: 26878150]
CCRF-CEM	ED₅₀	>50 μM Compound: beta-L-SddC (3TC)	In vitro concentration required to decrease 50% of mitochondrial DNA content in CEM cells In vitro concentration required to decrease 50% of mitochondrial DNA content in CEM cells	[PMID: 8627596]
CCRF-CEM	ED₅₀	50 μM Compound: beta-L-SddC (3TC)	In vitro concentration required to inhibit 50% of CEM cell growth In vitro concentration required to inhibit 50% of CEM cell growth	[PMID: 8627596]
HeLa	EC₅₀	>404 μM Compound: 36, FTC, Emtricitabine	Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay	[PMID: 22352809]
HeLa	EC₅₀	0.8 μM Compound: 36, FTC, Emtricitabine	Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay	[PMID: 22352809]
HeLa	EC₅₀	2 μM Compound: 36, FTC, Emtricitabine	Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay	[PMID: 22352809]
HeLa	IC₅₀	0.17 μM Compound: FTC	Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication	[PMID: 19596885]
HepG2	CC₅₀	765 μM Compound: FTC	Cytotoxicity against human HepG2 cells after 3 days by MTT assay Cytotoxicity against human HepG2 cells after 3 days by MTT assay	[PMID: 17404006]
HepG2	EC₅₀	0.03 μM Compound: FTC	Inhibition of hepatitis B virus replication in the HepAD38 cell line. Inhibition of hepatitis B virus replication in the HepAD38 cell line.	[PMID: 11128652]
HepG2	ED₅₀	17 nM Compound: beta-L-SddC (3TC)	Concentration required to inhibit 50% of extracellular circular replication of HBV DNA using 2215 cell line Concentration required to inhibit 50% of extracellular circular replication of HBV DNA using 2215 cell line	[PMID: 8627596]
HepG2	ED₅₀	30 nM Compound: beta-L-SddC (3TC)	Concentration required to inhibit 50% of intracellular circular replication of HBV DNA using 2215 cell line Concentration required to inhibit 50% of intracellular circular replication of HBV DNA using 2215 cell line	[PMID: 8627596]
HepG2	IC₅₀	27.7 μM Compound: emtricitabine	Cytotoxicity against human HepG2 cells after 9 days by MTT assay Cytotoxicity against human HepG2 cells after 9 days by MTT assay	[PMID: 17888662]
HepG2 2.2.15	EC₅₀	0.1 μM Compound: FTC	Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR	[PMID: 17404006]
HL-60	CC₅₀	845 μM Compound: FTC	Cytotoxicity against human HL60 cells after 3 days by MTT assay Cytotoxicity against human HL60 cells after 3 days by MTT assay	[PMID: 17404006]
MT2	EC₅₀	323 nM Compound: FTC	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	ED₅₀	2 μM Compound: beta-L-SddC (3TC)	Concentration required to inhibit 50% of HIV activity in MT-2 cells Concentration required to inhibit 50% of HIV activity in MT-2 cells	[PMID: 8627596]
MT2	IC₅₀	0.044 μM Compound: FTC	Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication	[PMID: 19596885]
PBMC	CC₅₀	>10 μM Compound: FTC	Cytotoxicity against human PBMC cells assessed as cell viability measured after 11 days by Viacount assay Cytotoxicity against human PBMC cells assessed as cell viability measured after 11 days by Viacount assay	[PMID: 34795872]
PBMC	CC₅₀	>200 μM Compound: 3; (-)-FTC	Cytotoxicity against PBMC (unknown origin) Cytotoxicity against PBMC (unknown origin)	[PMID: 37393791]
Vero	IC₅₀	>100 μM Compound: 51	Cytotoxicity was determined in the vero cells infected with HIV-I Cytotoxicity was determined in the vero cells infected with HIV-I	[PMID: 8423591]

In Vitro

Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC₅₀) ranges from 0.002 to 1.5 μ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine^[1].

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

In Vivo

Reproductive and developmental toxicology studies are conducted with emtricitabine. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC_0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine^[2].

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

Ensayo clínico

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

Chemical Information

No. CAS 143491-57-0
Appearance Solid
Peso molecular 247.25
Fòrmula C₈H₁₀FN₃O₃S
Color White to off-white
SMILES

O=C1N=C(N)C(F)=CN1[C@@H]2CS[C@H](CO)O2
Synonyms

BW1592
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (8)

All ELISAMicrobiological AssayWB

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Journal Impact Factor

Cell Rep Med

Decoupling HIV-1 antiretroviral drug inhibition from plasma antibody activity to evaluate broadly neutralizing antibody therapeutics and vaccines. [Abstract]

2024 Aug 26:101702. PMID: 39216479

Emtricitabine purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Aug 26:101702. [Abstract]

Inhibition of MuLV-pseudotyped HIV^pv-WT and HIV^pv-MDR viruses by different ARVs. Heatmap depicts mean inhibitory concentration 50 (IC₅₀) values from two independent experiments. Compound mix: efavirenz (EFV), Emtricitabine (FTC), dolutegravir (DTG), and darunavir (DRV) were combined and titrated.
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
ACS Infect Dis

Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]

2025 Oct 30. PMID: 41166549
J Neuroimmune Pharmacol

Antiretroviral Drugs Promote Amyloidogenesis by De-Acidifying Endolysosomes. [Abstract]

2021 Mar;16(1):159-168. PMID: 31338753

Emtricitabine purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]

Levels of Aβ _1-40 from the media of cultured neurons after ART compounds treatment for 48 h were detected by ELISA. Δ secreted Aβ_1-40 represented the difference of secreted Aβ_1-40 between ARTs and DMSO (vehicle controls). Lamivudine (1 μM), Emtricitabine (0.1 μM), tenofovir disoproxil (10 μM), ritonavir (1 μM), nelfinavir (1 μM), darunavir (0.1 μM), efavirenz (1 μM), nevirapine (1 μM), dolutegravir (1 μM) and elvitegravir (1 μM) significantly increased secreted Aβ_1-40, whereas zidovudine (10 μM) and abacavir (10 μM) significantly decreased secreted Aβ_1-40.
J Neuroimmune Pharmacol

Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. [Abstract]

2017 Dec;12(4):682-692. PMID: 28735382

Emtricitabine purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]

TDF/FTC (Emtricitabine)/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.
SSRN

2026 Jun 23.
bioRxiv

Mechanistic insights and in vivo HIV suppression by the BRD4-targeting small molecule ZL0580. [Abstract]

2025 Aug 14:2025.08.14.670267. PMID: 40832229
Open Virol J

Both Cyclophilin Inhibitors and Direct-Acting Antivirals Prevent PKR Activation in HCV-Infected Cells. [Abstract]

2014 Mar 7;8:1-8. PMID: 24799968

Emtricitabine purchased from MedChemExpress. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8. [Abstract]

The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor Emtricitabine). Results are representative of 4 independent experiments.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (404.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 25 mg/mL (101.11 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

4.0445 mL

20.2224 mL

40.4449 mL

5 mM

0.8089 mL

4.0445 mL

8.0890 mL

10 mM

0.4044 mL

2.0222 mL

4.0445 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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 (10.11 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 (10.11 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 (10.11 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.

Working solution concentration: 0.22 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) .

Protocolo

Cell Assay^[3]

EA.hy926 cells were plated in a 12-, 24- or 96-well plates and grown in DMEM media supplemented with 3% FCS. Endothelial cells from PARP^+/+and PARP^-/- mice were isolated and cultured. Cell viability was determined by the reduction of yellow MTT into a purple formazan product by mitochondrial dehydrogenases of metabolically active cells. Following the treatment period, the experimental medium was removed and 100 μL MTT (1 mg/mL) added. After 1 h incubation, the MTT solution was carefully removed and the purple crystals were solubilized in 100 μL of DMSO. The DMSO was transferred to an ELISA plate and absorbance measured at 550 nm with a 620 nm^[3].

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

Animal Administration^[2]

Mice: Emtricitabine (free base) is suspended in 0.5% aqueous methylcellulose and given by gavage, with the daily dose divided into two equal installments administered approximately 6 h apart. The dose volume is 5 mL/kg/dose (10 mL/kg/day). In 1- and 6-month oral toxicity studies in mice, the maximum tolerated dose of emtricitabine is >3000 mg/kg/day. However, dose-range-finding studies are performed in pregnant CD-1 mice and in New Zealand White rabbits at top doses of 1000 mg/kg/day^[2]. Rabbits: Mature artificially inseminated rabbits are given emtricitabine on gestational day 7 through 19. On gestational day 19, blood samples for toxicokinetics are taken from five satellite does in each group at 30–60 min prior to dosing, and at 1, 3, 7, and 12 h after the first daily-dose (prior to the second daily-dose). On gestational day 20, the satellite does are sacrificed at 1 h after the final dose, and maternal blood and fetal umbilical blood samples are collected for toxicokinetics^[2].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Saag MS, et al. Emtricitabine, a new antiretroviral agent with activity against HIV and hepatitis B virus. Clin Infect Dis.?2006 Jan 1;42(1):126-31. [Content Brief]

[2]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Content Brief]

[3]. Szczech GM, Wang LH, Walsh JP, Reproductive toxicology profile of emtricitabine in mice and rabbits. Reprod Toxicol. 2003 Jan-Feb;17(1):95-108. [Content Brief]

[4]. Faltz M, et al. Effect of the Anti-retroviral Drugs Efavirenz, Tenofovir and Emtricitabine on Endothelial Cell Function: Role of PARP. Cardiovasc Toxicol. 2017 Jan 3. [Epub ahead of print] [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	4.0445 mL	20.2224 mL	40.4449 mL	101.1122 mL
	5 mM	0.8089 mL	4.0445 mL	8.0890 mL	20.2224 mL
	10 mM	0.4044 mL	2.0222 mL	4.0445 mL	10.1112 mL
	15 mM	0.2696 mL	1.3482 mL	2.6963 mL	6.7408 mL
	20 mM	0.2022 mL	1.0111 mL	2.0222 mL	5.0556 mL
	25 mM	0.1618 mL	0.8089 mL	1.6178 mL	4.0445 mL
	30 mM	0.1348 mL	0.6741 mL	1.3482 mL	3.3704 mL
	40 mM	0.1011 mL	0.5056 mL	1.0111 mL	2.5278 mL
	50 mM	0.0809 mL	0.4044 mL	0.8089 mL	2.0222 mL
	60 mM	0.0674 mL	0.3370 mL	0.6741 mL	1.6852 mL
	80 mM	0.0506 mL	0.2528 mL	0.5056 mL	1.2639 mL
	100 mM	0.0404 mL	0.2022 mL	0.4044 mL	1.0111 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.

Keywords

Emtricitabine

8 Cited Publications

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Emtricitabine

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Publications Citing Use of MedChemExpress (MCE) Emtricitabine

Ver todos los productos específicos de isoformas HIV

Ver todos los productos específicos de isoformas Endogenous Metabolite

Actividad biológica

Chemical Information

Publications (8)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Emtricitabine Related Classifications

HY-17427 Related Classifications