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Deschloroclozapine

Cat. No. M11551
Deschloroclozapine  Structure
Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
25mg USD 155  USD155 In stock
50mg USD 255  USD255 In stock
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Quality Control & Documentation
Biological Activity

Deschloroclozapine is an effective, high affinity, selective, metabolically stable agonist based on muscarinic DREADDs. The Ki binding values of Deschloroclozapine to DREADD receptor subtypes hM3Dq and hM4Di were 6.3 and 4.2 nM, respectively.

Chemical Information
Molecular Weight 292.38
Formula C18H20N4
CAS Number 1977-07-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder -20°C
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] Todd B Nentwig, et al. Sci Rep. Behavioral and slice electrophysiological assessment of DREADD ligand, deschloroclozapine (DCZ) in rats

[2] Xuefeng Yan, et al. J Cereb Blood Flow Metab. [ 11 C]deschloroclozapine is an improved PET radioligand for quantifying a human muscarinic DREADD expressed in monkey brain

[3] Feng Hu, et al. Eur J Med Chem. 18 F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography

[4] Yuji Nagai, et al. Nat Neurosci. Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys

[5] Nicholas A Upright, et al. Neuropsychopharmacology. Effect of chemogenetic actuator drugs on prefrontal cortex-dependent working memory in nonhuman primates

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