Tenofovir alafenamide(GS-7340)

Molecular Weight (MW)	476.47
Formula	C21H29N6O5P
CAS No.	379270-37-8
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 95 mg/mL (199.4 mM)
Water:<1 mg/mL
Ethanol: 95 mg/mL (199.4 mM)
Other info	Chemical Name: (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate InChi Key: LDEKQSIMHVQZJK-AZFZMOAFSA-N InChi Code: InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33?/m1/s1 SMILES Code: C[C@H](N[P@@](OC1=CC=CC=C1)(CO[C@H](C)CN2C=NC3=C(N)N=CN=C23)=O)C(OC(C)C)=O
Synonyms	GS7340; GS-7340; GS 7340; Genvoya

Molecular Weight (MW)

476.47

Formula

C21H29N6O5P

CAS No.

379270-37-8

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 95 mg/mL (199.4 mM)

Water:<1 mg/mL

Ethanol: 95 mg/mL (199.4 mM)

Other info

Chemical Name: (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate
InChi Key: LDEKQSIMHVQZJK-AZFZMOAFSA-N
InChi Code: InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33?/m1/s1
SMILES Code: C[C@H](N[P@@](OC1=CC=CC=C1)(CO[C@H](C)CN2C=NC3=C(N)N=CN=C23)=O)C(OC(C)C)=O

Synonyms

GS7340; GS-7340; GS 7340; Genvoya

In Vitro	In vitro activity: GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP. Cell Assay: Tenofovir alafenamide antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT.
In Vivo	In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue.
Animal model	Beagle dogs
Formulation & Dosage	10 mg/kg, p.o.
References	Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1085-90; Antimicrob Agents Chemother. 2005 May;49(5):1898-906.

In Vitro

In vitro activity: GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP.

Cell Assay: Tenofovir alafenamide antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT.

In Vivo

In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue.

Animal model

Beagle dogs

Formulation & Dosage

10 mg/kg, p.o.

References

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1085-90; Antimicrob Agents Chemother. 2005 May;49(5):1898-906.

CAS NO:	379270-37-8
规格:	≥98%

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