R82913 (Synonyms: 9-Cl-TIBO)

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R82913 (9-Cl-TIBO) is a potent and high selective inhibitor of HIV-1 reverse transcriptase with antiviral activity on both an RNA template (negative strand synthesis) and a DNA template (positive strand synthesis). R82913 inhibits the replication of different strains of HIV-I in CEM cells with a median IC₅₀ value of of 0.15 μM.

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R82913 Chemical Structure

CAS No. : 126347-69-1

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
C8166	IC₅₀	0.0015 μM Compound: TIBO R-82913	Antiviral activity was evaluated by inhibition of HIV-1 replication in CD4+ lymphoblastoid cell line infected with HIV/IIIB strain Antiviral activity was evaluated by inhibition of HIV-1 replication in CD4+ lymphoblastoid cell line infected with HIV/IIIB strain	10.1016/0960-894X(95)00257-T
C8166	EC₅₀	0.002 μM Compound: R-82913	Tested against HIV-1 111B for Inhibition of viral replication by determining reduction of syncytia formation and antigen gp120 in C8166 cells, estimated by ELISA Tested against HIV-1 111B for Inhibition of viral replication by determining reduction of syncytia formation and antigen gp120 in C8166 cells, estimated by ELISA	10.1016/S0960-894X(97)00022-X
CEM-SS	IC₅₀	0.055 μM Compound: R-82913	Tested for the inhibition of HIV-1 in CEM-SS cells measured using Syncytial assay Tested for the inhibition of HIV-1 in CEM-SS cells measured using Syncytial assay	10.1016/S0960-894X(01)81224-5
CEM-SS	CC₅₀	35 μM Compound: R-82913	Tested for the cytotoxicity against CEM-SS cells (determined by the inhibition of [3H]-thymidine uptake) Tested for the cytotoxicity against CEM-SS cells (determined by the inhibition of [3H]-thymidine uptake)	10.1016/S0960-894X(01)81224-5
MOLT-4	IC₅₀	0.19 μM Compound: TIBO R-82913	Anti-HIV activity against HIV-1 in Molt-4 cells using 7-day infective assay Anti-HIV activity against HIV-1 in Molt-4 cells using 7-day infective assay	[PMID: 7506311]
MOLT-4	IC₅₀	19 μM Compound: TIBO R-82913	Tested for cytotoxicity in Molt-4 cells by XTT assay Tested for cytotoxicity in Molt-4 cells by XTT assay	[PMID: 7506311]

Molecular Weight

321.87

Formula

C₁₆H₂₀ClN₃S

CAS No.

126347-69-1

SMILES

S=C1N2C3=C(C=C(C=C3N1)Cl)CN([C@H](C2)C)C/C=C(C)\C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. White EL, et al. A TIBO derivative, R82913, is a potent inhibitor of HIV-1 reverse transcriptase with heteropolymer templates. Antiviral Res. 1991 Oct;16(3):257-66. [Content Brief]

[2]. Larder BA. 3'-Azido-3'-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 1992 Dec;36(12):2664-9. [Content Brief]

R82913 Related Classifications

Infection

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

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:

R82913126347-69-19-Cl-TIBOR 82913R-82913Reverse TranscriptaseHIVDNA/RNA SynthesisHuman immunodeficiency virusHIV-1 reverse transcriptaseantiviral activityRNA templateDNA templateCEM cellsInhibitorinhibitorinhibit

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