| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
pKi: 7.08 (M1), 7.78 (M2), 6.7(M3), 7(M4)
(S)-(+)-Dimethindene maleate targets histamine H1 receptors and muscarinic acetylcholine receptors (M2 subtype). It acts as a histamine H1 receptor antagonist with a pA2 of 7.8. It is also a potent M2-selective muscarinic receptor antagonist with pKi values of 7.08, 7.78, 6.70, and 7.00 for M1, M2, M3, and M4 receptors, respectively. |
|---|---|
| ln Vitro |
(S)-(+)-Dimethindene maleate (2 μM; 1 hour) transforms primed human pluripotent stem cells (hPSC) for the rapid differentiation of hEPS cells and greatly reduces the developmental capacity of mouse expanded pluripotent stem cells (mEPS) cells in chimeric blastocysts [2].
In vitro, (S)-(+)-Dimethindene maleate is a histamine H1 receptor antagonist with a pA2 of 7.8. It is a potent M2-selective muscarinic receptor antagonist with pA2 values of 7.86/7.74. The compound shows subtype-selective muscarinic receptor binding. |
| ln Vivo |
(S)-(+)-Dimethindene maleate shows affinity profile at muscarinic M1 (NB-OK 1 cells), M2 (rat heart), M3 (rat pancreas) and M4 receptors (rat striatum), with pKis 7.08, 7.78, 6.7 and 7,respectively[1]. |
| Enzyme Assay |
The in vitro receptor binding assay for (S)-(+)-Dimethindene maleate involves measuring its affinity for histamine H1 and muscarinic receptors. Radioligand binding assays are performed using membrane preparations from cells expressing the receptors. The compound's pA2 and pKi values are determined by competitive displacement of labeled ligands.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Mouse EPS cells Tested Concentrations: 2 μM Incubation Duration: 1 hour Experimental Results: Dramatically impaired the developmental potency of mEPS cells. Cellular assays for (S)-(+)-Dimethindene maleate are performed using cells expressing histamine H1 or muscarinic receptors. Cells are treated with the compound and stimulated with histamine or a muscarinic agonist. Receptor activation is assessed by measuring downstream signaling events such as calcium mobilization. |
| Animal Protocol |
In vivo animal studies for (S)-(+)-Dimethindene maleate are not detailed in the available sources. The compound is an approved antihistamine drug. Preclinical studies would have been conducted in animal models of allergy and inflammation.
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| ADME/Pharmacokinetics |
(S)-(+)-Dimethindene maleate is administered orally or topically. It has a molecular weight of 408.49 g/mol. The compound is soluble in DMSO. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
(S)-(+)-Dimethindene maleate is generally well-tolerated. Common side effects include drowsiness, dry mouth, and dizziness. As an antihistamine, it may cause sedation. Specific toxicological data are not provided in the supplier documentation.
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| References | |
| Additional Infomation |
(S)-(+)-Dimethindene maleate is an antihistamine drug used for the treatment of allergies and skin irritation. It is a chiral compound that is the (S)-(+)-enantiomer of dimethindene. The compound is also a potent M2-selective muscarinic receptor antagonist. It is available from chemical suppliers for research purposes.
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| Molecular Formula |
C24H28N2O4
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|---|---|
| Molecular Weight |
408.490126609802
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| Exact Mass |
408.204
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| CAS # |
136152-65-3
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| Related CAS # |
(R)-(+)-Dimethindene maleate;136152-64-2;Dimethindene maleate;3614-69-5;Dimethindene;5636-83-9
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| PubChem CID |
56972160
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
518
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN(C)C.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
SWECWXGUJQLXJF-HFNHQGOYSA-N
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| InChi Code |
InChI=1S/C20H24N2.C4H4O4/c1-15(19-10-6-7-12-21-19)20-17(11-13-22(2)3)14-16-8-4-5-9-18(16)20;5-3(6)1-2-4(7)8/h4-10,12,15H,11,13-14H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-;/m1./s1
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| Chemical Name |
(Z)-but-2-enedioic acid;N,N-dimethyl-2-[3-[(1S)-1-pyridin-2-ylethyl]-1H-inden-2-yl]ethanamine
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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 (~244.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.90 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 20.0 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 mg/mL (4.90 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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 mg/mL (4.90 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 | 2.4480 mL | 12.2402 mL | 24.4804 mL | |
| 5 mM | 0.4896 mL | 2.4480 mL | 4.8961 mL | |
| 10 mM | 0.2448 mL | 1.2240 mL | 2.4480 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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