Rifapentine (DL 473)

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
500mg	$290	Check With Us
1g	$470	Check With Us
5g	$1175	Check With Us

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Cat #: V2329 CAS #: 61379-65-5 Purity ≥ 98%

Description: Rifapentine (formerly also known as MDL473; Priftin; DL 473, Cyclopentylrifampicin) is a potent antibiotic/antimicrobial of the rifamycin class, used to treat tuberculosis. It inhibits DNA-dependent RNA polymerase activity. Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both Rifapentine and its active metabolite, 25-desacetylrifapentine, localize within monocyte-derived macrophages, thus allowing for intracellular inhibition of M. tuberculosis at a greater kill rate as compared with that of the parent or metabolite alone. Rifapentine is deacetylated in the liver and induces cytochrome P450 much less than rifampin.

References: [1]. Sharma, S.K., et al., Rifamycins (rifampicin, rifabutin and rifapentine) compared to isoniazid for preventing tuberculosis in HIV-negative people at risk of active TB. Cochrane Database Syst Rev, 2013. 7: p. CD007545.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	877.03
Molecular Formula	C47H64N4O12
CAS No.	61379-65-5
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 100 mg/mL (114.0 mM)r
	Water: <1 mg/mLr
	Ethanol: 17 mg/mL (19.4 mM)
SMILES Code	CO[C@H]1/C=C/O[C@]2(Oc(c(C)c3O)c(C2=O)c4c3c(O)c(NC(/C(C)=C\C=C\[C@@H]([C@@H]([C@H]([C@H]([C@H]([C@@H]([C@@H]1C)OC(C)=O)C)O)C)O)C)=O)c(/C=N/N5CCN(C6CCCC6)CC5)c4O)C
Synonyms	MDL473; MDL 473; MDL-473; DL 473; DL-473; DL473; R 773; R-773; R773;

Protocol	In Vitro	In vitro activity: The activities of rifampin and rifapentine against Mycobacterium tuberculosis residing in human monocytederived macrophages were determined. The MIC and MBC of rifapentine for intracellular bacteria were two- to four-fold lower than those of rifampin. For extracellular bacteria, this difference was less noticeable. Cell Assay: Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both Rifapentine and its active metabolite, 25-desacetylrifapentine, localize within monocyte-derived macrophages, thus allowing for intracellular inhibition of M. tuberculosis at a greater kill rate as compared with that of the parent or metabolite alone. Rifapentine is deacetylated in the liver and induces cytochrome P450 much less than rifampin. Rifapentine has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages.
	In Vivo	Rifapentine inhibits bacterial RNA synthesis by binding to the β-subunit of DNA-dependent RNA polymerase in susceptible species. Rifapentine is generally more active than rifampicin against sensitive strains of M. tuberculosis. Rifapentine significantly increases the rate of antipyrine and pentobarbital metabolism in vivo. Rifapentine also increases liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase. Rifapentine combined with isoniazid (INH) and pyrazinamide (PZA) administered daily results in an apparent clearance of M.tuberculosis organisms in the lungs and spleens of infected mice after 10 weeks of treatment
	Animal model	Mice

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.1402 mL	5.7011 mL	11.4021 mL	22.8042 mL
5mM	0.2280 mL	1.1402 mL	2.2804 mL	4.5608 mL
10mM	0.1140 mL	0.5701 mL	1.1402 mL	2.2804 mL
20mM	0.0570 mL	0.2851 mL	0.5701 mL	1.1402 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.