1. Anti-infection
  2. HIV
  3. ZLM-66

ZLM-66 

Cat. No.: HY-150769
Handling Instructions

ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS.

For research use only. We do not sell to patients.

ZLM-66 Chemical Structure

ZLM-66 Chemical Structure

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Description

ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS[1].

IC50 & Target[1]

HIV-1 (WT)

13 nM (EC50)

HIV-1 (K103N)

13 nM (EC50)

HIV-1 (L100I)

24 nM (EC50)

HIV-1 (E138K)

25 nM (EC50)

HIV-1 (Y181C)

58 nM (EC50)

HIV-1 (K103N+Y181C)

260 nM (EC50)

HIV-1 (F227L+V106A)

27530 nM (EC50)

In Vitro

ZLM-66 (0.0016-125 µg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells[1].

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

Cell Viability Assay[1]

Cell Line: MT-4 cells infected with WT HIV-1 strain (IIIB) or HIV-2 (ROD)
Concentration: 125, 25, 5, 1, 0.2, 0.04, 0.008 and 0.0016 µg/ml
Incubation Time: 5 d
Result: Exbited EC50 value, CC50 value and SI value of 13 nM, 26.45 μM and 2019.8 respectively against HIV-1 (IIIB). Inhibited L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, and K103N + Y181C (single and double HIV mutant strains) with EC50s of 24, 13, 58, 760, 25, 27530 and 260 nM, respectively.
In Vivo

Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration[1].
1.19 Pharmacokinetic Parameters of ZLM-66 in rat[1].

/tr> /tr>
Rat
IV 1 mg/kg
Rat
PO 5 mg/kg
T1/2 (h) 1.90±0.28 8.45±4.88
Tmax (h) 0.08±0.00 6.67±1.15
Cmax (ng/mL) 468.67±63.09 583.33±290.11
AUC0-t (h*ng/ml) 891.94±79.30 4983.22±3220.11
AUC0-∞ (h*ng/ml) 940.41±105.00 6594.05±1547.74
CL (ml/h/kg) 1072.31±120.40 791.14±210.66
MRT0-t (h) 2.03±0.2 6.79±1.90
MRT0-∞ (h) 2.48±0.35 13.92±6.44
F (%) 140.24

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

Animal Model: Six- to 8-week-old male Sprague-Dawley rats (180−230 g)[1]
Dosage: 1, 5 mg/kg
Administration: Intravenous injection, oral gavage; 1-5 mg/kg; once
Result: Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.
Molecular Weight

481.43

Formula

C24H18F3N5O3

SMILES

CN1C(CN(C=CC(C(F)(F)F)=C2OC3=CC(C#N)=CC(C4=CC(C)=CC=C4)=C3)C2=O)=NNC1=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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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.

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ZLM-66
Cat. No.:
HY-150769
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