Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
Rilpivirine HCl (TMC-278; R-278474 HCl; DB-08864; Edurant; Rekambys; Cabenuva), the hydrochloride salt of Rilpivirine, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been approved for the treatment of HIV-1 infections. Rilpivirine is usually used in combination with other anti-HIV drugs such as cabotegravir (trade name Cabenuva for the combination of cabotegravir+Rilpivirine, approved in 2021).
ln Vitro |
R278474 is effective against all studied single and double mutants (EC50=0.1-2.0 nM) as well as HIV-1 wild-type (EC50=0.4 nM) [1]. R278474 (10-5000 nM; 30 d) Over the course of 30 days, no indication of a breakthrough of wild-type HIV-1 at 1 μM was seen [1]. At an inhibitory concentration (EC50) of less than 1 nM, R278474 inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) and 94% at an EC50 of less than 10 nM [1]. When it comes to wild-type HIV-1 M component isolates, TMC278 has subnanomolar EC50 values (0.07–1.01 nM) [2].
|
||
---|---|---|---|
ln Vivo |
Rats treated with R278474 (10-160 mg/kg; po for 1 month) do not exhibit any aberrant effects, with the exception of increased liver weight and species-specific thyroid hypertrophy at higher dose levels[1]. AUCinf values for R278474 (iv) range from 3.1 μg h/mL (4 mg/kg) in rats, 8.7 μg h/mL (1.25 mg/kg) in dogs, 1.4 μg h/mL (1.25 mg/kg) in monkeys, and 44 μg h/mL (1.25 mg/kg) in rabbits. Elimination half-lives range from 4.4 h in rats to 31 h in dogs[1]. In rats and dogs, R278474 (po) had half-live ranges of 2.8 and 39 hours, respectively, with oral bioavailability of 32% and 31%[1].
|
||
Animal Protocol |
|
||
References |
[1]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5.
[2]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [3]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. |
Molecular Formula |
C22H19CLN6
|
|
---|---|---|
Molecular Weight |
402.88
|
|
CAS # |
700361-47-3
|
|
Related CAS # |
Rilpivirine;500287-72-9;Rilpivirine-d6 hydrochloride;2714324-67-9
|
|
SMILES |
Cl.N#C/C=C/C1C=C(C)C(NC2C=CN=C(NC3C=CC(C#N)=CC=3)N=2)=C(C)C=1
|
|
InChi Key |
KZVVGZKAVZUACK-BJILWQEISA-N
|
|
InChi Code |
InChI=1S/C22H18N6.ClH/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19;/h3-9,11-13H,1-2H3,(H2,25,26,27,28);1H/b4-3+;
|
|
Chemical Name |
(E)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile hydrochloride
|
|
Synonyms |
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4821 mL | 12.4106 mL | 24.8213 mL | |
5 mM | 0.4964 mL | 2.4821 mL | 4.9643 mL | |
10 mM | 0.2482 mL | 1.2411 mL | 2.4821 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.