Referencia número: HY-14266

Dapivirine

(Synonyms: TMC120; R147681)

2 Cited Publications

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.80%
No. CAS: 244767-67-7
Fòrmula: C₂₀H₁₉N₅
Peso molecular:329.41

Almacenamiento:

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

Dapivirine Chemical Structure

No. CAS: 244767-67-7

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (2)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target

HIV-1

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Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	5 μM Compound: DAPIVIRINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	0.73 μM Compound: DAPIVIRINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
Macrophage	CC₅₀	>20000 nM Compound: dapivirine	Cytotoxicity against human monocyte derived macrophages after 24 hrs by MTT assay Cytotoxicity against human monocyte derived macrophages after 24 hrs by MTT assay	[PMID: 19029331]
MRC5	IC₅₀	>64 μM Compound: 1, TMC120	Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs	[PMID: 25199582]
MRC5	IC₅₀	1.25 μM Compound: 1, TMC120	Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay	[PMID: 25199582]
MT2	CC₅₀	2 μM Compound: 8a, TMC120	Cytotoxicity against human MT2 cells assessed as growth inhibition Cytotoxicity against human MT2 cells assessed as growth inhibition	[PMID: 23937980]
MT2	EC₅₀	0.039 μM Compound: 8a, TMC120	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.039 μM Compound: 8a, TMC120	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.0007 μM Compound: 8a, TMC120	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.7 nM Compound: 8a, TMC120	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	CC₅₀	1.9 μM Compound: TMC120	Cytotoxicity against human MT2 cells after 5 days by MTT assay Cytotoxicity against human MT2 cells after 5 days by MTT assay	[PMID: 24900627]
MT4	IC₅₀	>10 μM Compound: 13a	Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.001 μM Compound: 13a	Inhibitory activity against LAI strain of HIV-I in MT-4 cells Inhibitory activity against LAI strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.0043 μM Compound: 13a	Inhibitory activity against 103N strain of HIV-I in MT-4 cells Inhibitory activity against 103N strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.0075 μM Compound: 13a	Inhibitory activity against 181C strain of HIV-I in MT-4 cells Inhibitory activity against 181C strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.018 μM Compound: 13a	Inhibitory activity against 100I strain of HIV-I in MT-4 cells Inhibitory activity against 100I strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.044 μM Compound: 13a	Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	IC₅₀	0.048 μM Compound: 13a	Inhibitory activity against 188L strain of HIV-I in MT-4 cells Inhibitory activity against 188L strain of HIV-I in MT-4 cells	[PMID: 11527705]
MT4	EC₅₀	>10 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.001 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.004 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.008 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.018 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.044 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	EC₅₀	0.048 μM Compound: 13a	Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells	[PMID: 15771411]
MT4	CC₅₀	2150 nM Compound: dapivirine	Cytotoxicity against human MT4 cells after 24 hrs by MTT assay Cytotoxicity against human MT4 cells after 24 hrs by MTT assay	[PMID: 19029331]
MT4	IC₅₀	0.9 nM Compound: dapivirine	Antiviral activity against HIV-1 3B infected in human MT4 cells after 7 days by RT assay Antiviral activity against HIV-1 3B infected in human MT4 cells after 7 days by RT assay	[PMID: 19029331]
MT4	CC₅₀	3035.8 nM Compound: TMC120	Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay	[PMID: 21438533]
MT4	EC₅₀	0.03 nM Compound: TMC120	Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 21438533]
MT4	EC₅₀	0.3 nM Compound: TMC120	Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 21438533]
MT4	EC₅₀	1.2 nM Compound: TMC120	Antiviral activity against HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 21438533]
MT4	EC₅₀	1.2 nM Compound: TMC120	Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 21438533]
MT4	EC₅₀	333.9 nM Compound: TMC120	Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV 1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 21438533]
MT4	EC₅₀	0.6 nM Compound: TMC120	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22428851]
MT4	EC₅₀	1.2 nM Compound: TMC120	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22428851]
MT4	EC₅₀	1.2 nM Compound: TMC120	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22428851]
MT4	EC₅₀	330 nM Compound: TMC120	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22428851]
MT4	CC₅₀	3 μM Compound: TMC120	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 22428851]
MT4	EC₅₀	1.2 nM Compound: 8a, TMC120	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced effect Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced effect	[PMID: 23937980]
MT4	EC₅₀	54 nM Compound: 8a, TMC120	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced effect Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced effect	[PMID: 23937980]
MT4	EC₅₀	7 nM Compound: 8a, TMC120	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced effect Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced effect	[PMID: 23937980]
MT4	CC₅₀	2 μM Compound: TMC120	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	[PMID: 24805780]
MT4	EC₅₀	>20 μM Compound: TMC120	Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	>20 μM Compound: TMC120	Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.001 μM Compound: TMC120	Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.002 μM Compound: TMC120	Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.003 μM Compound: TMC120	Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.003 μM Compound: TMC120	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.04 μM Compound: TMC120	Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.05 μM Compound: TMC120	Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.1 μM Compound: TMC120	Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in	[PMID: 24805780]
MT4	EC₅₀	0.1 μM Compound: TMC120	Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.2 μM Compound: TMC120	Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	CC₅₀	3 μM Compound: TMC120	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	[PMID: 30525601]
TZM	CC₅₀	20400 nM Compound: dapivirine	Cytotoxicity against human TZM-bl cells after 24 hrs by MTT assay Cytotoxicity against human TZM-bl cells after 24 hrs by MTT assay	[PMID: 19029331]
TZM	CC₅₀	>0.304 μM Compound: TMC-120	Cytotoxicity against human TZM-bl cells Cytotoxicity against human TZM-bl cells	[PMID: 19666220]
TZM	CC₅₀	2.88 μM Compound: 6, TMC120, Dapivirine	Cytotoxicity against human TZM-b1 cells infected with wild type HIV1 BaL after 48 hrs using formazan dye by WST1 assay Cytotoxicity against human TZM-b1 cells infected with wild type HIV1 BaL after 48 hrs using formazan dye by WST1 assay	[PMID: 21930388]
TZM	CC₅₀	2.47 μM Compound: 1, TMC120	Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay	[PMID: 25199582]
TZM	CC₅₀	3.4 μM Compound: TMC120	Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 2 days by WST-1 assay Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 2 days by WST-1 assay	[PMID: 26898379]

In Vitro

Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h)^[1].
Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells^[1].
Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells^[1].
Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration^[3].

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

Cell Proliferation Assay^[1]

Cell Line:

U87 glioblastoma cells.
Concentration:

4, 8, 16 μM.
Incubation Time:

24, 48, 72, 96 and 120 hours.
Result:

Inhibited proliferation of glioma cells.
IC₅₀ was 10.73 μM.

Apoptosis Analysis^[1]

Cell Line:

U87 glioblastoma cells.
Concentration:

16 μM.
Incubation Time:

12h, 24h and 48h.
Result:

Induced apoptosis.
Decreased caspase-3.

In Vivo

Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice^[1].
Dapivirine has been shown to have a half-life in the range of 65 to 90 h^[4].

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

Animal Model:

U87 cells were subcutaneously injected into the nude mice^[1].
Dosage:

16 mg/kg.
Administration:

Once every 3 days for 12 days.
Result:

Significantly decreased the tumor volumes.
A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.

Ensayo clínico

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

Chemical Information

No. CAS 244767-67-7
Appearance Solid
Peso molecular 329.41
Fòrmula C₂₀H₁₉N₅
Color White to off-white
SMILES

CC1=CC(C)=CC(C)=C1NC2=CC=NC(NC3=CC=C(C#N)C=C3)=N2
Synonyms

TMC120; R147681
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 (2)

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Int J Antimicrob Agents

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

2019 Dec;54(6):814-819. PMID: 31479744
Sci Rep

NMR characterization of HIV-1 reverse transcriptase binding to various non-nucleoside reverse transcriptase inhibitors with different activities. [Abstract]

2015 Oct 29;5:15806. PMID: 26510386

Solvente y solubilidad

In Vitro:

DMSO : ≥ 47 mg/mL (142.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" 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

3.0358 mL

15.1788 mL

30.3576 mL

5 mM

0.6072 mL

3.0358 mL

6.0715 mL

10 mM

0.3036 mL

1.5179 mL

3.0358 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.

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: 2.08 mg/mL (6.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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μL
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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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Referencias

[1]. Weiwen Liu, et al. Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. J Cancer. 2018 Jan 1;9(1):117-128. [Content Brief]

[2]. Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8. [Content Brief]

[3]. Yven Van Herrewege, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. [Content Brief]

[4]. Michael E Halwes, et al. Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Eur J Pharm Sci. 2016 Oct 10;93:410-8. [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
DMSO	1 mM	3.0358 mL	15.1788 mL	30.3576 mL	75.8940 mL
	5 mM	0.6072 mL	3.0358 mL	6.0715 mL	15.1788 mL
	10 mM	0.3036 mL	1.5179 mL	3.0358 mL	7.5894 mL
	15 mM	0.2024 mL	1.0119 mL	2.0238 mL	5.0596 mL
	20 mM	0.1518 mL	0.7589 mL	1.5179 mL	3.7947 mL
	25 mM	0.1214 mL	0.6072 mL	1.2143 mL	3.0358 mL
	30 mM	0.1012 mL	0.5060 mL	1.0119 mL	2.5298 mL
	40 mM	0.0759 mL	0.3795 mL	0.7589 mL	1.8973 mL
	50 mM	0.0607 mL	0.3036 mL	0.6072 mL	1.5179 mL
	60 mM	0.0506 mL	0.2530 mL	0.5060 mL	1.2649 mL
	80 mM	0.0379 mL	0.1897 mL	0.3795 mL	0.9487 mL
	100 mM	0.0304 mL	0.1518 mL	0.3036 mL	0.7589 mL

Keywords

Dapivirine

2 Cited Publications

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Dapivirine

Anti-Infection Compound Library

Apoptosis Compound Library

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Antiviral Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

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Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

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Publications Citing Use of MedChemExpress (MCE) Dapivirine

Ver todos los productos específicos de isoformas HIV

Actividad biológica

Chemical Information

Publications (2)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Dapivirine

Anti-Infection Compound Library

Apoptosis Compound Library

Clinical Compound Library

Antiviral Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Cell Death 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

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Drug Fragment Library

Publications Citing Use of MedChemExpress (MCE) Dapivirine

Ver todos los productos específicos de isoformas HIV

Actividad biológica

Chemical Information

Publications (2)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Dapivirine Related Classifications

HY-14266 Related Classifications