| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
Taniborbactam (VNRX-5133) is a parenteral, potential best-in-class, reversible, specific boronic acid-containing compound that inhibits both serine- and metallo-β-lactamases with IC50s of 8-530 nM. Combined with cefepime, a fourth generation cephalosporin antibiotic, taniborbactam drives antimicrobial activity against gram-negative bacteria that have acquired multi-drug resistance (MDR) via classes A, B, C and D β-lactamase expression. Taniborbactam is the only known β-lactamase inhibitor in advanced clinical development that blocks class B carbapenemases. In 2019, Everest Medicines and licensing partner Venatorx Pharmaceuticals initiated a global Phase 3 clinical trial for patients with complicated urinary tract infections (cUTI).
| ln Vitro |
Taniborbactam (VNRX-5133) has an IC50 of 0.5 nM, 2 nM, 0.5 nM, and 0.06 against strains of Klebsiella pneumoniae, OXA-48, VIM-4, and VIM-2 of Pseudomonas aeruginosa. nM[2]. The combinations of cefepime/Taniborbactam (10 μg/mL) and meropenem/Taniborbactam demonstrated good efficacy against each of the six clinical isolates of Klebsiella pneumoniae and E that produced NDM-1. coli, with MICs varying from 1 -0.125 μg/mL to 16 to 0.25 μg/mL, respectively[1].
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|---|---|
| ln Vivo |
Mice that produced CTX-M-14 were given a single dose of cefepime (32 mg/kg)/Taniborbactam (VNRX-5133; 16 mg/kg; subcutaneously) in a neutropenic mouse lung infection model. injection) can reduce the number of Klebsiella pneumoniae strains by >4 log10 live bacterial counts [2]. When cefepime (16 mg/kg) and taniborbactam (16 mg/kg) were administered subcutaneously twice a day for seven days, the kidneys of an ascending urinary tract infection model exhibited greater activity than when CTX was used alone. More than two log10 fewer bacteria were found in -M-15-producing E. strains of Coli [2]. T1/2, CL, and Vss of taniborbactam in mice are 0.16 hours, 618 mL/h/kg, and 143 mL/kg, respectively[2].
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| References | |
| Additional Infomation |
Taniborbactam is under investigation in clinical trial NCT03840148 (Safety and Efficacy Study of Cefepime/vnrx-5133 in Patients With Complicated Urinary Tract Infections).
|
| Molecular Formula |
C19H28BN3O5
|
|---|---|
| Molecular Weight |
389.2537
|
| Exact Mass |
389.212
|
| CAS # |
1613267-49-4
|
| Related CAS # |
Taniborbactam hydrochloride;2244235-49-0
|
| PubChem CID |
76902493
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
544
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
B1([C@H](CC2=C(O1)C(=CC=C2)C(=O)O)NC(=O)CC3CCC(CC3)NCCN)O
|
| InChi Key |
PFZUWUXKQPRWAL-OFCDMGMCSA-N
|
| InChi Code |
InChI=1S/C19H28BN3O5/c21-8-9-22-14-6-4-12(5-7-14)10-17(24)23-16-11-13-2-1-3-15(19(25)26)18(13)28-20(16)27/h1-3,12,14,16,22,27H,4-11,21H2,(H,23,24)(H,25,26)/t12-,14-,16?
|
| Chemical Name |
(R)-3-(2-((1r,4R)-4-((2-aminoethyl)amino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylic
acid
|
| Synonyms |
VNRX-5133 VNRX5133 VNRX 5133
|
| HS Tariff Code |
2934.99.9001
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5690 mL | 12.8452 mL | 25.6904 mL | |
| 5 mM | 0.5138 mL | 2.5690 mL | 5.1381 mL | |
| 10 mM | 0.2569 mL | 1.2845 mL | 2.5690 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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