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Ticlopidine HCl 53885-35-1

Product Description

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Molecular Weight: 300.25 Ticlopidine HCl is an P2 Receptor Inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.

Ticlopidine HCl is an antiplatelet drug in the thienopyridine family.
Ticlopidine HCl inhibits platelet aggregation by altering the function
of platelet membranes by blocking ADP receptors. This prevents the
conformational change of glycoprotein IIb/IIIa which allows platelet
binding to fibrinogen. Ticlopidine HCl inhibits platelet
aggregation and prostaglandin synthesis from endogenous substrate
through activating basal and PGE1-stimulated activity of the cyclase,
preventing PGE2-induced depression of the cyclase activity and thus
increasing platelet c-AMP level.

Ticlopidine HCl inhibits platelet aggregation with IC50 of ~2 μM in men. Ticlopidine HCl, when orally administered to rats, results in
activation of basal and prostaglandin E1 (PGE1)-stimulated adenylate
cylase activity through increase in affinity of the cyclase in platelet
membrane to PGE1, although it failed to affect adenosine- or sodium
fluoride-stimulated activity of the enzyme.






Protocol(Only for Reference)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) 300.25
Formula

C14H14ClNS.HCl

CAS No. 53885-35-1

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



Solubility (25°C) * In vitro DMSO 1 mg/mL (3.33 mM)
Water 4 mg/mL (13.32 mM)
Ethanol 1 mg/mL (3.33 mM)





Chemical Name 5-[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridine, hydrochloride (1:1)










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Product Categories : Neuronal Signaling > P2 Receptor Inhibitor