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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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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].
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| 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].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited information indicates that maternal rilpivirine doses of 25 mg daily produce low levels in milk and infant serum. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. Achieving and maintaining viral suppression with antiretroviral therapy decreases breastfeeding transmission risk to less than 1%, but not zero. Individuals with HIV who are on antiretroviral therapy with a sustained undetectable viral load and who choose to breastfeed should be supported in this decision. If a viral load is not suppressed, banked pasteurized donor milk or formula is recommended. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| Additional Infomation |
Rilpivirine hydrochloride is a hydrochloride obtained by reaction of rilpivirine with one equivalent of hydrochloric acid. Used for treatment of HIV. It has a role as a prodrug, a HIV-1 reverse transcriptase inhibitor and an EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor. It contains a rilpivirine(1+).
Rilpivirine (brand names: Edurant and Edurant PED) is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for use with other HIV medicines for the treatment of HIV infection in adults and children 2 years of age and older who weigh at least 31 lb (14 kg) who have never taken HIV medicines before and who meet certain requirements, as determined by a health care provider. Rilpivirine (brand name: Edurant) is also FDA-approved for use with oral cabotegravir (brand name: Vocabria) for the short-term treatment of HIV infection in adults and children 12 years of age and older who weigh at least 77 lb (35 kg) and who meet certain requirements, as determined by a health care provider. A diarylpyrimidine derivative and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 that is used in the treatment of HIV INFECTIONS. It is also used in combination with other ANTI-HIV AGENTS, since ANTIVIRAL DRUG RESISTANCE emerges rapidly when it is used alone. See also: Rilpivirine (has active moiety); Dolutegravir sodium; rilpivirine hydrochloride (component of) ... View More ... Drug Indication Edurant, in combination with other antiretroviral medicinal products, is indicated for the treatment of human immunodeficiency virus type 1 (HIVâ1) infection in antiretroviral treatmentânaïve patients 12 years of age and older with a viral load ⤠100,000 HIVâ1 RNA copies/ml. , , As with other antiretroviral medicinal products, genotypic resistance testing should guide the use of Edurant. , Treatment of human immunodeficiency virus (HIV-1) infection |
| Molecular Formula |
C22H19CLN6
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| Molecular Weight |
402.88
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| Exact Mass |
402.136
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| CAS # |
700361-47-3
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| Related CAS # |
Rilpivirine;500287-72-9;Rilpivirine-d6 hydrochloride;2714324-67-9
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| PubChem CID |
11711114
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| Appearance |
White to off-white solid powder
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| LogP |
5.285
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
607
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)/C=C/C#N.Cl
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| InChi Key |
KZVVGZKAVZUACK-BJILWQEISA-N
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| 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+;
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| Chemical Name |
(E)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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