Efavirenz
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 5g | $180 | Check With Us |
| 10g | $280 | Check With Us |
| 20g | $420 | Check With Us |
: Cat #: V2641 CAS #: 154598-52-4 Purity ≥ 98%
Description: Efavirenz (also called Sustiva, Stocrin, DMP-266, DMP 266), a non-nucleoside reverse transcriptase inhibitor (NNRTI), is a highly potent and specific inhibitor of human immunodeficiency virus type 1 reverse transcriptase with Ki value of 2.93nM.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
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- Quality Control Documentation
| Molecular Weight (MW) | 315.67 |
|---|---|
| Molecular Formula | C14H9ClF3NO2 |
| CAS No. | 154598-52-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 63 mg/mL (199.6 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 63 mg/mL (199.6 mM) | |
| Synonyms | DMP-266, DMP 266; Efavirenz; Sustiva; Stocrin; DMP-266; DMP 266; trade name: efavirenz; L-743,726; L-743726; DMP266; EFV; L 743726 |
| Protocol | In Vitro | Efavirenz (L-743726) is found to be capable of inhibiting, with 95% inhibitory concentrations of ≤ 1.5μM, a panel of nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs)-resistant mutant viruses, each of which expresses a single RT amino acid substitution. Efavirenz is also tested for its activity against a variety of polymerase enzymes and is found to be inactive (IC50>300μM). Efavirenz effectively inhibits several wild-type T-lymphoid cell line-adapted variants. Identical activity (IC95, 1.5 to 3.0 nM) is seen with wild-type primary isolates of the virus in both primary lymphoid and monocytoid cell cultures. Efavirenz also effectively inhibits HIV-1 variants that expressed RT amino acid substitutions which confer the loss of susceptibility to other NNRTIs. For purposes of comparison. |
|---|---|---|
| In Vivo | After i.v. administration, Efavirenz (L-743726) is cleared rapidly from rats, but it is cleared considerably more slowly from monkeys. The large volume of distribution (two to four times the amount of body water) in both species indicates extensive tissue binding. The oral bioavailability in rats is 16%. In monkeys, the half-life of Efavirenz after administration of a 1 mg/kg i.v. dose exceeded 2.5 h. Efavirenz is well absorbed orally. Administration to monkeys of oral doses as fine suspensions in 0.5% aqueous methylcellulose yields consistently high levels in plasma. A 2.0 mg/kg dose produces peak levels of 0.5μM at approximately 3.0 h. The absolute bioavailability is estimated to be 42%. A 10 mg/kg dose yields a peak level in plasma of 3.22 μM. A 10 mg/kg oral dose given to a single chimpanzee gave concentrations in plasma of 4.12, 2.95, and 2.69 μM at 2, 8, and 24 h after dosing, respectively |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.1679 mL | 15.8393 mL | 31.6787 mL | 63.3573 mL |
| 5mM | 0.6336 mL | 3.1679 mL | 6.3357 mL | 12.6715 mL |
| 10mM | 0.3168 mL | 1.5839 mL | 3.1679 mL | 6.3357 mL |
| 20mM | 0.1584 mL | 0.7920 mL | 1.5839 mL | 3.1679 mL |
| Quality Control Documentation |
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The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.