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[CAS NO. 473921-12-9] Lersivirine
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-14267 |
| Brand: | MCE |
| CAS: | 473921-12-9 |
Overview
| MDL | MFCD16619314 |
|---|---|
| Molecular Weight | 310.35 |
| Molecular Formula | C17H18N4O2 |
| SMILES | CCC1=NN(CCO)C(CC)=C1OC2=CC(C#N)=CC(C#N)=C2 |
Summary
Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC 50 =119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains [1] .
IC50 & Target
IC50: 119 nM (NNRT) [1]
In Vitro
Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01254656 | Pfizer|ViiV Healthcare |
HIV-1
|
February 2011 | Phase 2 |
| NCT01220232 | Pfizer|ViiV Healthcare |
Healthy Volunteers
|
November 2010 | Phase 1 |
| NCT01099748 | Pfizer |
Healthy Volunteers
|
May 2010 | Phase 1 |
| NCT01050751 | Pfizer |
Healthy Volunteers
|
February 2010 | Phase 1 |
| NCT01603485 | Pfizer|ViiV Healthcare |
Healthy Volunteer
|
June 2012 | Phase 1 |
| NCT00925535 | Pfizer |
Healthy Volunteers
|
May 2010 | Phase 1 |
| NCT01230385 | Pfizer|ViiV Healthcare |
Healthy Volunteers
|
October 2010 | Phase 1 |
| NCT00936871 | Pfizer |
Healthy Volunteers
|
January 2010 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 161.11 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL |
| 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL |
-
1.
References
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