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DREADD agonist 21

Cat. No. M11552
DREADD agonist 21  Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 185  USD185 In stock
25mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

DREADD Agonist 21 is an effective agonist for human muscarinic acetylcholine M3 receptor (hM3Dq) (EC50=1.7 nM).

Chemical Information
Molecular Weight 278.35
Formula C17H18N4
CAS Number 56296-18-5
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Valrie Van Steenbergen, et al. Exp Neurol. Chemogenetic approaches to unravel circuit wiring and related behavior after spinal cord injury

[2] Wei Guo, et al. Brain Res Bull. Abnormalities in the composition of the gut microbiota in mice after repeated administration of DREADD ligands

[3] R Maldonado, et al. Neuropharmacology. Vulnerability to addiction

[4] Martin Jendryka, et al. Sci Rep. Pharmacokinetic and pharmacodynamic actions of clozapine-N-oxide, clozapine, and compound 21 in DREADD-based chemogenetics in mice

[5] Karen J Thompson, et al. ACS Pharmacol Transl Sci. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo

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