Elvitegravir free base

Elvitegravir is an HIV integrase inhibitor.

For research use only. Not for human or veterinary use.

Target HIV IntegraseHIV

Research area Infection

Purity >98% Stock Inquire

Data Sheet SDS COA

Elvitegravir structure

CAS No.: 697761-98-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 450.00	BP-02494-500mg	In stock	Get quote
1 g	USD 685.00	BP-02494-1g	In stock	Get quote
5 g	USD 1,250.00	BP-02494-5g	In stock	Get quote
10 g	USD 1,849.00	BP-02494-10g	In stock	Get quote

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Description

Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

Biological activity

Elvitegravir also inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir (also known as JTK-303/GS-9137) blocked the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. EVG inhibited the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. The replication capacity of EVG-resistant variants was significantly reduced relative to both wild-type virus and other IN inhibitor-resistant variants selected by L-870810. Elvitegravir (GS-9137) is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells. According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor. Elvitegravir is currengly in a Phase III clinical trial in the treatment of HIV-1 Infection.

Identifiers

SMILES: COC1=C(CC2=CC=CC(Cl)=C2F)C=C2C(=O)C(=CN([C@H](CO)C(C)C)C2=C1)C(O)=O
InChIKey: JUZYLCPPVHEVSV-LJQANCHMSA-N

Specifications

MW (average): 447.8840
Formula: C₂₃H₂₃ClFNO₅
CAS No.: 697761-98-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 6 months

Solubility

Soluble in DMSO

Documents

References

[1].Shimura K, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74.

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