Rilpivirine HCl (TMC278; DB08864)

Alias: TMC-278;R-278474 HCl; DB-08864;DB08864, TMC278;D08864; TMC-278;R-278474;Edurant; Rekambys; Cabenuva; R-278474, R278474, D08864, TMC 278; Rilpivirine HCl; Edurant.
Cat No.:V2143 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 thetreatment ofHIV-1 infections.
Rilpivirine HCl (TMC278; DB08864) Chemical Structure CAS No.: 700361-47-3
Product category: Reverse Transcriptase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Rilpivirine HCl (TMC278; DB08864):

  • Rilpivirine (R278474; TMC278)
  • Rilpivirine-d6 hydrochloride
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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).

Biological Activity I Assay Protocols (From Reference)
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
Dissolved in PEG 400; 4 mg/kg ( rat); 1.25 mg/kg (other species); i.v. or p.o.
Sprague Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H19CLN6
Molecular Weight
402.88
CAS #
700361-47-3
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
TMC-278;R-278474 HCl; DB-08864;DB08864, TMC278;D08864; TMC-278;R-278474;Edurant; Rekambys; Cabenuva; R-278474, R278474, D08864, TMC 278; Rilpivirine HCl; Edurant.
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 Data
Solubility (In Vitro)
DMSO: 73 mg/mL (199.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

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.

Contact Us