MK-1439
Doravirine
CAS: 1338225-97-0
Molecular Formula: C17H11ClF3N5O3
MK-1439 - Names and Identifiers
MK-1439 - Physico-chemical Properties
| Molecular Formula | C17H11ClF3N5O3 |
| Molar Mass | 425.75 |
| Melting Point | >278°C (dec.) |
| Solubility | DMSO: ≥ 30 mg/mL |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | -20°C Freezer |
| Use | Doravirine (MK-1439) is a highly specific HIV-1 non-nucleoside reverse transcriptase inhibitor. The IC50 values for wild type and K103N and Y181C reverse transcriptase mutants are 4.5 nM,5.5 nM and 6.1 nM, respectively. |
| In vitro study | MK-1439 have an IC50 greater than 100 μm for DNA polymerases α, ß, and γ in the cell. In the 110 protein target (including enzymes, transporters, ion channels and receptors) screening, MK-1439 IC50 values for most targets are greater than 10 μm, except for 5-HT2β, its IC50 value was MK-1429 to be 2.5 μm in the ligand binding assay. However, in experiments measuring the accumulation of inositol-1-phosphate in cells, no 5-HT2ß activity was detected. In activated CD4 T cells, peripheral blood mononuclear cells, macrophage proliferation of transformed cell lines, the concentration of up to 100 M MK-1439 without cytotoxicity. |
| In vivo study | In rats, administered by intravenous injection (1 mg/kg), the MK-1439 has a plasma clearance of 5.4 mL/min/kg and a half-life of 4.4 hours, the volume of distribution was 2.3 L/kg. The oral bioavailability was 57% with 5 mg/kg administered by oral route. In beagle dogs, a plasma clearance of 0.36 mL/min/kg with a half-life of 37 hours was achieved by intravenous injection of 0.5 mg/kg of MK-1439. The oral bioavailability of MK-1439 in Beagle dogs was 52% at 1 mg/kg by oral route. |
MK-1439 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.349 ml | 11.744 ml | 23.488 ml |
| 5 mM | 0.47 ml | 2.349 ml | 4.698 ml |
| 10 mM | 0.235 ml | 1.174 ml | 2.349 ml |
| 5 mM | 0.047 ml | 0.235 ml | 0.47 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Doravirine Request for quotation
CAS: 1338225-97-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
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CAS: 1338225-97-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Doravirine Visit Supplier Webpage Request for quotationCAS: 1338225-97-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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