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Technical Data
| Formula | C20H19N5 |
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| Molecular Weight | 329.4 | CAS No. | 244767-67-7 | |
| Solubility (25°C)* | In vitro | DMSO | 34 mg/mL (103.21 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Dapivirine (TMC120) is a non-nucleoside inhibitor 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. Phase 3. | ||
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| In vitro | Dapivirine prevents HIV-induced syncytium formation in the nanomolar range and shows a low cytostatic activity. Dapivirine apparently blocks HIV-1 infection in the primary cultures at a 10 nM concentration, but secondary cultures reveals that a 100 nM concentration is needed to completely prevent proviral integration. [1] Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells. [2] | ||
| In vivo | Dapivirine-containing gel at vaginal level inhibits cell-associated HIV infection in mice. [3] More placebo (7 of 12) than Dapivirine (3 of 24) gel users has positive vaginal swab results, with white blood cells being the most common finding. Dapivirine (0.05%) results in Cmax of 715 pg/mL, AUC of 15 ng×h/mL and T1/2 of 89.87 hours in plasma after 14 days post-dose. Mean Dapivirine (0.05%) concentrations in vaginal fluids collected at the introitus, mid vagina, and cervix are in the range of 62-265 μg/g on day 1. [4] |
Protocol (from reference)
References
Selleck's Dapivirine (TMC120) has been cited by 11 publications
| Comprehensive Study of Antiretroviral Drug Permeability at the Cervicovaginal Mucosa via an In Vitro Model [ Pharmaceutics, 2022, 14(9)1938] | PubMed: 36145684 |
| Female Genital Fibroblasts Diminish the In Vitro Efficacy of PrEP against HIV [ Viruses, 2022, 14(8)1723] | PubMed: 36016345 |
| Impact of vaginal microbiome communities on HIV antiretroviral-based pre-exposure prophylaxis (PrEP) drug metabolism [ PLoS Pathog, 2020, 16(12):e1009024] | PubMed: 33270801 |
| Reciprocal Modulation of Antiretroviral Drug and Steroid Receptor Function In Vitro. [ Antimicrob Agents Chemother, 2019, 64(1)] | PubMed: 31658973 |
| Combination of G2-S16 dendrimer/dapivirine antiretroviral as a new HIV-1 microbicide. [ Future Med Chem, 2019, 11(23):3005-3013] | PubMed: 31710246 |
| Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. [ J Cancer, 2018, 9(1):117-128] | PubMed: 29290776 |
| In Silico and in Vitro Screening for P-Glycoprotein Interaction with Tenofovir, Darunavir, and Dapivirine: An Antiretroviral Drug Combination for Topical Prevention of Colorectal HIV Transmission. [ Mol Pharm, 2017, 14(8):2660-2669] | PubMed: 28648081 |
| In Vitro Cross-Resistance Profiles of Rilpivirine, Dapivirine, and MIV-150, Nonnucleoside Reverse Transcriptase Inhibitor Microbicides in Clinical Development for the Prevention of HIV-1 Infection. [ Antimicrob Agents Chemother, 2017, 61(7)] | PubMed: 28507107 |
| Drug transporter gene expression in human colorectal tissue and cell lines: modulation with antiretrovirals for microbicide optimization. [ J Antimicrob Chemother, 2016, 71(2):372-86] | PubMed: 26514157 |
| Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans [ Eur J Pharm Sci, 2016, 93:410-8] | PubMed: 27559026 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.