2. Anti-infection
  3. HIV Reverse Transcriptase
  4. HIV-1 inhibitor-49

HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model.

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HIV-1 inhibitor-49 Chemical Structure

HIV-1 inhibitor-49 Chemical Structure

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HIV-1 inhibitor-49 Related Antibodies

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Description

HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model[1].

IC50 & Target[1]

HIV-1 (WT)

17 nM (EC50)

HIV-1 (L100I)

0.38 μM (EC50)

HIV-1 (K103N)

2.64 μM (EC50)

HIV-1 (Y181C)

1.85 μM (EC50)

HIV-1 (E138K)

0.09 μM (EC50)

In Vitro

HIV-1 inhibitor-49 (compound 9h) (EC50=17 nM-39.21 μM) inhibits WT HIV-1 with much higher selectivity index over other HIV-1 mutant (L100I, K103N, Y181C, and E138K)[1].
HIV-1 inhibitor-49 (0-50 μM) shows little CYP enzyme, hERG inhibition in CHO-hERG cells, with IC50s of 27.6 μM (CYP2C9), 30.3 μM (CYP2C19), and >50 μM (others)[1].

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

HIV-1 inhibitor-49 Related Antibodies
In Vivo

HIV-1 inhibitor-49 (compound 9h) (1000 mg/kg; i.g.; single dose) does not induce mice death and obvious pathological damage in healthy mouse model[1].
HIV-1 inhibitor-49 (10 mg/kg; p.o.; single dose) shows excellent oral bioavailability in rats[1].

Rat PK profile[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) T1/2 (h) Tmax (h) Vz (mL/kg) Cl (mL/h/kg) Cmax (ng/mL) F (%)
i.v. 1.0 1102 1100 0.514 0.083 698 936 2033
p.o. 10 9557 8663 2.51 0.583 3523 86.72%

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

416.44

Formula

C21H18F2N2O3S
SMILES

O=C1NC(N(C(SC2=CC(F)=CC=C2F)=C1C3CC3)COCC4=CC=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HIV-1 inhibitor-49 Related Classifications

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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:

HIV-1 inhibitor-49HIVReverse TranscriptaseHuman immunodeficiency virusInhibitorinhibitorinhibit

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