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| 5mg |
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| 10mg |
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| 25mg |
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Sofpironium bromide (formerly BBI-4000; BBI-4000; Ecclock) is a potent anticholinergic drug approved in Japan in 2020 as a 5% gel for the treatment of primary axillary hyperhidrosis (excessive underarm sweating). Sofpironium bromide is a new chemical entity belonging to the class of medications called anticholinergics. Anticholinergics block the action of acetylcholine, a chemical that transmits signals within the nervous system that are responsible for a range of bodily functions, including activation of the sweat glands. Sofpironium bromide was retrometabolically designed. It reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site, and exhibits high affinity for the M1, M2, M4 and M5 muscarinic receptor subtypes.
| ln Vitro |
In addition to undergoing oxidative metabolism through CYP2D6 and CYP3A4, sopironium bromide is mostly metabolized by non-enzymatic hydrolysis [1].
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| ln Vivo |
By reducing the contractile activity of guinea pig ileal tissue in a concentration-dependent manner, sofpironium bromide demonstrates anticholinergic action. In a rat model, solopidium bromide decreased footpad sweating caused by the muscarinic receptor agonist pilocarpine [1].
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| References |
| Molecular Formula |
C22H32BRNO5
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|---|---|
| Molecular Weight |
470.397186279297
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| Exact Mass |
469.146
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| CAS # |
1628106-94-4
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| Related CAS # |
1628251-49-9 (cation);1628106-94-4 (bromide);
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| PubChem CID |
86301316
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
555
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| Defined Atom Stereocenter Count |
2
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| SMILES |
[Br-].O(C([C@](C1C=CC=CC=1)(C1CCCC1)O)=O)[C@@H]1CC[N+](C)(CC(=O)OCC)C1
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| InChi Key |
FIAFMTCUJCWADZ-JOFREBOKSA-M
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| InChi Code |
InChI=1S/C22H32NO5.BrH/c1-3-27-20(24)16-23(2)14-13-19(15-23)28-21(25)22(26,18-11-7-8-12-18)17-9-5-4-6-10-17;/h4-6,9-10,18-19,26H,3,7-8,11-16H2,1-2H3;1H/q+1;/p-1/t19-,22+,23?;/m1./s1
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| Chemical Name |
3-((R)-2-cyclopentyl-2-hydroxy-2-phenylacetoxy)-1-(2-ethoxy-2-oxoethyl)-1-methylpyrrolidin-1-ium bromide
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| Synonyms |
BBI4000 Ecclock BBI-4000 Sofpironium bromide
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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 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~212.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.31 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 (5.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (5.31 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 | 2.1259 mL | 10.6293 mL | 21.2585 mL | |
| 5 mM | 0.4252 mL | 2.1259 mL | 4.2517 mL | |
| 10 mM | 0.2126 mL | 1.0629 mL | 2.1259 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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