Dapivirine (TMC120)Nonnucleoside reverse transcriptase inhibitor CAS# 244767-67-7 |
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Quality Control & MSDS
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| Cas No. | 244767-67-7 | SDF | Download SDF |
| PubChem ID | 214347 | Appearance | Powder |
| Formula | C20H19N5 | M.Wt | 329.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | TMC120; R147681 | ||
| Solubility | DMSO : ≥ 47 mg/mL (142.68 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile | ||
| SMILES | CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C | ||
| Standard InChIKey | ILAYIAGXTHKHNT-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H19N5/c1-13-10-14(2)19(15(3)11-13)24-18-8-9-22-20(25-18)23-17-6-4-16(12-21)5-7-17/h4-11H,1-3H3,(H2,22,23,24,25) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Dapivirine (TMC120) is a non-nucleoside inhibitor of HIV reverse transcriptase with an IC50 vaule of 24 nM. | |||||
| Targets | HIV reverse transcriptase | |||||
| IC50 | 24 nM | |||||
Dapivirine (TMC120) Dilution Calculator
Dapivirine (TMC120) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0358 mL | 15.1791 mL | 30.3582 mL | 60.7165 mL | 75.8956 mL |
| 5 mM | 0.6072 mL | 3.0358 mL | 6.0716 mL | 12.1433 mL | 15.1791 mL |
| 10 mM | 0.3036 mL | 1.5179 mL | 3.0358 mL | 6.0716 mL | 7.5896 mL |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.2143 mL | 1.5179 mL |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.6072 mL | 0.759 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Dapivirine (DPV) is a nonnucleoside reverse transcriptase inhibitor with a favorable safety profile following vaginal application.
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Safety and availability of dapivirine (TMC120) delivered from an intravaginal ring.[Pubmed:19388819]
AIDS Res Hum Retroviruses. 2009 May;25(5):483-8.
Vaginal delivery of 200 mg or 25 mg dapivirine from intravaginal rings (IVRs) was evaluated over a 7-day period in two phase 1 safety trials (IPM001 and IPM008, respectively) in a total of 25 healthy women 19 to 46 years of age. The IVR was generally safe and well tolerated with similar adverse events observed in the placebo and dapivirine groups. Across both studies, dapivirine concentrations in vaginal fluids measured at the introitus, cervix, and ring area were within the mean range of 0.7-7.1 microg/ml. Mean dapivirine concentrations in vaginal and cervical tissues on day 7 were 0.3-0.7 microg/g in IPM001 and 1.5-3.5 microg/g in IPM008. Mean plasma concentrations of dapivirine were <50 pg/ml. Dapivirine from both IVRs was successfully distributed throughout the lower genital tract at concentrations >1000x the EC(50) against wild-type HIV-1 (LAI) in MT4 cells suggesting that IVR delivery of microbicides is a viable option meriting further study.
Dapivirine(TMC 120, TMC 120 R147681) is a NNRTI for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates.
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