| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
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| Other Sizes |
| Targets |
Coccidia; MRSA; VRE
|
|---|---|
| ln Vitro |
Robenidine (compound 1) inhibits MRSA and VRE growth, with minimum inhibitory concentrations (MIC) of 8.1 and 4.7 μM, respectively. Robenidine exhibits bactericidal effects on all strains of Staphylococcus aureus with an MBC/MIC90 ratio of less than two. Robenidine was found to have no activity in 50% serum, but to have a significant negative impact on MIC values in 2% serum, with a 4-fold decrease [1].
|
| ln Vivo |
The mean plasma concentrations in the florfenicol (FFC) alone group exceeded 1 µg/mL after about 6 hours; this was lowered to 4 hours after a pretreatment of Robenidine (ROB). In rabbits given a pretreatment of robenidine, the terminal elimination half-life (t1/2z), area under the concentration-time curve (AUC), area under the first moment curve (AUMC), and mean residence time (MRT) all significantly decreased, while the elimination rate constant (λz) and systemic Clearance rate (CLz) increased [2].
|
| Animal Protocol |
Drug Interaction Study Design:** Thirty-two healthy New Zealand White male rabbits (2-2.5 kg) were divided into four groups (n=8 per group). The control group was fed anticoccidial-free rations throughout the study. The treatment groups were fed rations containing Robenidine (66 ppm), sulfaquinoxaline (250 ppm), or toltrazuril (2 ppm) for 20 consecutive days. At the end of the 20th day of feeding, a single dose of florfenicol (25 mg/kg body weight) was injected intravenously into the left auricular vein of each rabbit. Blood samples (approximately 1 ml) were collected from the right auricular vein at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 4, 6, 8, and 12 hours after florfenicol administration. Plasma was harvested by centrifugation and stored at -20°C until analysis [1].
* **Pharmacokinetic Analysis:** Plasma florfenicol concentrations were determined by HPLC. Pharmacokinetic parameters were calculated using non-compartmental analysis based on statistical moment theory. Parameters included elimination rate constant (λz), terminal elimination half-life (t₁/₂z), area under the concentration-time curve (AUC), area under the first moment curve (AUMC), mean residence time (MRT), total body clearance (CLz), and apparent steady-state volume of distribution (Vss) [1]. |
| References | |
| Additional Infomation |
type of anticoccidial drug primarily used in poultry.
See also: robenidin (containing the active component); chlorotetracycline; robenidin hydrochloride (component); bacitracin zinc; robenidin hydrochloride (component)...see more... Robenidin, 1 (2,2'-bis[(4-chlorophenyl)methylene]carboimine dihydrazide), is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), with minimum inhibitory concentrations (MICs) of 8.1 μM and 4.7 μM, respectively. Structure-activity relationship studies showed that the 4-chloroisostrain was resistant to 4-fluoro(8), 3-fluoro(9), 3-chloro(22) and 4-chlorocarbon(27) (23.7-71 μM) as well as 3-chloro(3), 4-chloro(21) and 4-chlorocarbon(26) (8.1-13.0 μM). Imine carbon alkylation revealed a methyl/ethyl binding pocket that also accommodates a CH₂OH group (75; 2,2'-bis[1-(4-chlorophenyl)-2-hydroxyethyl]carboimide dihydrazide). Analogs 1, 27 (2,2'-bis{[4-(1,1-dimethylethyl)phenyl]methylene}carboimide dihydrazide) and 69 (2,2'-bis[1-(4-chlorophenyl)ethyl]carboimide dihydrazide hydrochloride) were active against 24 clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA). No dose-limiting cytotoxicity at ≥2×MIC or hemolysis at ≥8×MIC was observed. With the addition of polymyxin B, the MICs for activity against Gram-negative Escherichia coli and Pseudomonas aeruginosa ranged from 4.2 to 21.6 μM. Compounds 1 and 75 exhibited excellent microsomal stability, intrinsic clearance, and liver extractability in both human and mouse liposomes, with T1/2 > 247 min, CLint < 7 μL/min/mg protein, and EH < 0.22; Compound 75 also exhibited excellent microsomal stability, intrinsic clearance, and liver extractability in human liposomes. [1] |
| Molecular Formula |
C15H14CL3N5
|
|---|---|
| Molecular Weight |
370.66
|
| Exact Mass |
369.031
|
| Elemental Analysis |
C, 48.61; H, 3.81; Cl, 28.69; N, 18.89
|
| CAS # |
25875-50-7
|
| Related CAS # |
Robenidine-d8 hydrochloride;1173097-77-2
|
| PubChem CID |
16212175
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
488.1ºC at 760 mmHg
|
| Melting Point |
252-254°C
|
| Flash Point |
249ºC
|
| Vapour Pressure |
1.12E-09mmHg at 25°C
|
| LogP |
5.158
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
408
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CC=C1/C=N/N/C(=N/N=C/C2=CC=C(C=C2)Cl)/N)Cl.Cl
|
| InChi Key |
LTWIBTYLSRDGHP-HCURTGQUSA-N
|
| InChi Code |
InChI=1S/C15H13Cl2N5.ClH/c16-13-5-1-11(2-6-13)9-19-21-15(18)22-20-10-12-3-7-14(17)8-4-12;/h1-10H,(H3,18,21,22);1H/b19-9+,20-10+;
|
| Chemical Name |
1,2-bis[(E)-(4-chlorophenyl)methylideneamino]guanidine;hydrochloride
|
| Synonyms |
Robenidine hydrochloride; Cycostat; Robenidine HCl; 25875-50-7; Robenzidine; Robenidine hydrochloride [USAN]; 8STT15Y392; UNII-8STT15Y392; Robenidine-d8 HCl;ChimcoccideRobenidine HCl
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~6.25 mg/mL (~16.86 mM)
H2O : ~1 mg/mL (~2.70 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.62 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6979 mL | 13.4895 mL | 26.9789 mL | |
| 5 mM | 0.5396 mL | 2.6979 mL | 5.3958 mL | |
| 10 mM | 0.2698 mL | 1.3489 mL | 2.6979 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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