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(S)-(+)-Dimethindene maleate

Cat. No. M25486
(S)-(+)-Dimethindene maleate Structure
Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 220  USD220 In stock
25mg USD 480  USD480 In stock
50mg USD 820  USD820 In stock
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Quality Control & Documentation
Biological Activity

(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48). (S)-(+)-Dimethindene maleate (2 μM; 1 h) significantly impaires the developmental potency of mouse extended pluripotent stem (mEPS) cells in chimeric blastocysts and leads to rapid differentiation of primed human pluripotent stem cell (hPSC)-converted hEPS cells.

Chemical Information
Molecular Weight 408.49
Formula C24H28N2O4
CAS Number 136152-65-3
Solubility (25°C) DMSO 90 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Junjun Xu, et al. Stem Cell Res Ther. Generation of pig induced pluripotent stem cells using an extended pluripotent stem cell culture system

[2] Yang Yang, et al. Cell. Derivation of Pluripotent Stem Cells with In Vivo Embryonic and Extraembryonic Potency

[3] Thomas M Böhme, et al. J Med Chem. Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists

[4] O Pfaff, et al. Eur J Pharmacol. The (S)-(+)-enantiomer of dimethindene: a novel M2-selective muscarinic receptor antagonist

[5] F Humphreys, et al. Br J Clin Pharmacol. The effect of topical dimethindene maleate on weal reactions

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