| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
After oral dosing (13.2 for mice, 20 for rats, and 5 mg/kg for dogs), zamifenacin has moderate oral bioavailability (26% in mice, 64% in rats, and 100% in dogs) and Cmax (92 in mice, 905 in rats, and 416 ng/mL in dogs) [2]. Large distribution volume (12.5, 19.0, and 3.5 L/kg after intravenous injection; 5.3 in mice, 5.0 in rats, and 1.0 mg/dog in dogs, respectively) and high plasma clearance (68, 35, and 39 mL/min/kg, respectively) are the reasons for this [2].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Male CD1 mice (average weight 23g) [2]
Doses: 5.3 mg/kg, intravenous (iv) (iv)injection; oral 13.2 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)administration and oral administration Experimental Results: oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (2.1 h). Animal/Disease Models: Male and female CD rats (average body weight 210 g) [2] Doses: 5.0 mg/kg, intravenous (iv) (iv)injection; oral 20 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)administration and oral administration Experimental Results: Oral bioavailability (64%), Cmax (905 ng/mL) , T1/2 (6.0 h). Animal/Disease Models: Male and two female beagle dogs (13-16 kg) [2] Doses: 1.0 mg/kg intravenously (iv) (iv)(iv); 5 mg/kg orally (pharmacokinetic/PK/PK analysis) Mode of Route of Administration: intravenous (iv) (iv)and oral administration Experimental Results: Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h). |
| References |
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| Additional Infomation |
(3R)-1-[2-(1,3-benzodioxol-5-yl)ethyl]-3-(diphenylmethyl)oxypiperidine is a diarylmethane.
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| Molecular Formula |
C27H29NO3
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|---|---|
| Molecular Weight |
415.533
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| Exact Mass |
415.215
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| CAS # |
127308-82-1
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| Related CAS # |
Zamifenacin fumarate;127308-98-9
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| PubChem CID |
3086618
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2g/cm3
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| Boiling Point |
532.5ºC at 760mmHg
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| Flash Point |
145.6ºC
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| LogP |
5.166
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
513
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C[C@H](CN(C1)CCC2=CC3=C(C=C2)OCO3)OC(C4=CC=CC=C4)C5=CC=CC=C5
|
| InChi Key |
BDNFQGRSKSQXRI-XMMPIXPASA-N
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| InChi Code |
InChI=1S/C27H29NO3/c1-3-8-22(9-4-1)27(23-10-5-2-6-11-23)31-24-12-7-16-28(19-24)17-15-21-13-14-25-26(18-21)30-20-29-25/h1-6,8-11,13-14,18,24,27H,7,12,15-17,19-20H2/t24-/m1/s1
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| Chemical Name |
(3R)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine
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| Synonyms |
UK-76654; UK76654; UK 76654
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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 : ~100 mg/mL (~240.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.02 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 25.0 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: 2.5 mg/mL (6.02 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4066 mL | 12.0328 mL | 24.0657 mL | |
| 5 mM | 0.4813 mL | 2.4066 mL | 4.8131 mL | |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4066 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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