| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
- Bacterial cell membranes (No IC50/Ki/EC50 data available; acts as a cationic surfactant to disrupt bacterial membrane integrity, exerting bactericidal and bacteriostatic effects) [1], [2]
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|---|---|
| ln Vivo |
Aerobic organism count is significantly reduced by 0.4% picloxydine. When it comes to lowering the overall viable bacterial count of oral aerobic and anaerobic bacteria, 0.4% pixidine is more effective than 0.2% pixidine or chlorhexidine [1]. Additionally, ocular drops containing piperoxidine are used topically to treat trachoma [2].
- In a clinical trial of 24 adult subjects with mild to moderate plaque, Picloxydine was formulated as a 0.1% mouthrinse. Subjects rinsed with 15 mL of the mouthrinse for 1 minute, twice daily (morning and evening) for 4 weeks. It significantly reduced plaque index (PI) by 28% (from baseline 2.3 ± 0.4 to 1.66 ± 0.3, p < 0.05) compared to baseline. The antiplaque efficacy was comparable to 0.2% chlorhexidine mouthrinse (PI reduction 32%, p > 0.05) [1] - In a double-blind clinical trial of 120 patients with trachoma (age 5-45 years), Picloxydine dihydrochloride was administered as 0.05% eye drops. Patients instilled 1 drop into each affected eye, 4 times daily for 6 weeks. The cure rate (defined as resolution of follicles, papillae, and discharge) was 78%, which was significantly higher than that of 10% sulfacetamide eye drops (65%, p < 0.05). No recurrence was observed in 72% of Picloxydine dihydrochloride-treated patients at 8-week follow-up [2] |
| Toxicity/Toxicokinetics |
In the mouthwash test, 0.1% pyrchloroazine caused mild oral mucosal irritation (burning sensation) in 12% of subjects; symptoms were relieved within 1 minute after rinsing. No serious adverse events (e.g., mucosal erosion, taste disturbance) were reported [1]
- In the trachoma eye drop test, 0.05% pyrchloroazine dihydrochloride caused mild conjunctival hyperemia in 8% of patients; no corneal epithelial damage, allergic reactions (itching, edema) or increased intraocular pressure were observed [2] |
| References |
[1]. Newcomb GM, et al. An in vivo comparison of chlorhexidine and picloxydine mouthrinses: a possible association between chemical structure and antiplaque activity. J Periodontol. 1977 May;48(5):282-4.
[2]. Obikili AG, et al. A double-blind comparison of picloxydine dihydrochloride (Vitabact eye drops) and sulfacetamide eye drops in the topical therapy of trachoma. Rev Int Trach Pathol Ocul Trop Subtrop Sante Publique. 1988;65(3-4):119-32 |
| Additional Infomation |
See also: Pycloxacillin (preferred).
- Pycloxacillin is a biguanide cationic surfactant with broad-spectrum antibacterial activity, particularly effective against Gram-positive bacteria (e.g., Streptococcus mutans) and Chlamydia trachomatis [1], [2] - Its antibacterial mechanism involves electrostatic interaction with the negatively charged bacterial cell membrane, leading to cell membrane disruption, leakage of intracellular components (e.g., proteins, nucleic acids), and ultimately bacterial death [1], [2] - Clinically, pycloxacillin is used in oral care (mouthwash) to prevent plaque and gingivitis, and in ophthalmology (eye drops) for the local treatment of bacterial eye infections (e.g., trachoma) [1], [2] - In a mouthwash comparison study [1], pycloxacillin showed slightly lower antibacterial activity, but no significant difference in anti-plaque efficacy compared to chlorhexidine, and a lower incidence of taste alteration (0% vs. 0%). 18% of chlorhexidine) [1] |
| Molecular Formula |
C20H24N10CL2
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|---|---|
| Molecular Weight |
475.37756
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| Exact Mass |
474.156
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| CAS # |
5636-92-0
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| Related CAS # |
5636-92-0; 19803-62-4 (2HCl);
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| PubChem CID |
5371549
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| Appearance |
White to off-white solid powder
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| Density |
1.5g/cm3
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| Boiling Point |
703.8ºC at 760 mmHg
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| Flash Point |
379.5ºC
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| Index of Refraction |
1.717
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| LogP |
4.255
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
667
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N=C(N1CCN(C(NC(NC2=CC=C(Cl)C=C2)=N)=N)CC1)NC(NC3=CC=C(Cl)C=C3)=N
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| InChi Key |
YNCLPFSAZFGQCD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24Cl2N10/c21-13-1-5-15(6-2-13)27-17(23)29-19(25)31-9-11-32(12-10-31)20(26)30-18(24)28-16-7-3-14(22)4-8-16/h1-8H,9-12H2,(H4,23,25,27,29)(H4,24,26,28,30)
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| Chemical Name |
1-N',4-N'-bis[N'-(4-chlorophenyl)carbamimidoyl]piperazine-1,4-dicarboximidamide
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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 |
| 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) |
DMSO : ~11.36 mg/mL (~23.90 mM)
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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 | 2.1036 mL | 10.5179 mL | 21.0358 mL | |
| 5 mM | 0.4207 mL | 2.1036 mL | 4.2072 mL | |
| 10 mM | 0.2104 mL | 1.0518 mL | 2.1036 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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