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Home > Products > Neuronal Signaling > AChR Inhibitor > Diphemanil Methylsulfate 62-97-5

Diphemanil Methylsulfate 62-97-5

Product Description

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Molecular Weight: 389.51 Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).

Diphemanil Methylsulfate exerts its action by primarily binding the
muscarinic M3 receptor. In addition to its well known antimuscarinic
effects, Diphemanil Methylsulfate also possesses direct smooth muscle
spasmolytic activity.

The pharmacokinetic experiments show that absorption of diphemanil
methylsulphate is slow (tmax = 2 to 4 h), the mean half-life is 8.35 h,
and the amount of the drug recovered in urine within 48 h ranges from
0.6 to 7.4% of the administered dose. Poorly absorbed from the gastrointestinal tract with an absolute bioavailability of 15 to 25%.



Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)










Chemical Information




Molecular Weight (MW) 389.51
Formula

C20H24N.CH3O4S

CAS No. 62-97-5

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 25 mg/mL (64.18 mM)
Water 28 mg/mL (71.88 mM)
Ethanol <1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.




Chemical Name Piperidinium, 4-(diphenylmethylene)-1,1-dimethyl-, methyl sulfate (1:1)







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