JDS364
JDS364 is a blood-brain barrier-permeable human acetylcholinesterase (hAChE) reactivator with an IC50 of 8.6 μM. JDS364 achieves rapid systemic exposure in mice and acts as a protective agent when used in combination with Atropine (HY-B1205). JDS364 can be used in studies on organophosphate nerve agent poisoning and organophosphate pesticide poisoning.
For research use only. We do not sell to patients.
- CAS No.: 2072857-15-7
- Formula: C19H20N4O2
- Molecular Weight:336.39
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
hAChE 8.6 μM (IC50) |
In Vitro
JDS364 demonstrates broad-spectrum, high-efficiency reactivation of hAChE inhibited by nerve agent surrogates and paraoxon, with exceptional efficacy against tabun surrogate-inhibited hAChE[1].
JDS364 (50 μM) exhibits high permeability across a validated human in vitro BBB model without causing cytotoxicity or barrier disruption, confirming its potential for CNS penetration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Tmax | MRT |
|---|---|---|---|---|
| Mice[1] | 100 μmol/Kg | i.p. | 4.5 min | 33.1 min |
In Vivo
JDS364 (100 μmol/kg; i.p.; single dose) exhibits rapid and efficient functional bioavailability in mouse blood, reaching peak reactivation capacity within 5 minutes of intraperitoneal administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Swiss mice (male, 9 weeks old, 35-45 g)[1]
-
Dosage:100 μmol/kg (monotherapy); 100 μmol/kg + 10 mg/kg atropine (combination therapy)
-
Administration:i.p.; single dose; 1 minute post-agent challenge
-
Result:Achieved a protective index (PI) of 2.6 against paraoxon, 1.3 against NIMP, and 1.5 against NEMP when administered alone.
Exhibited a PI of 6.7 against paraoxon, 2.7 against NIMP, and 3.7 against NEMP when combined with atropine.
Had a median lethal dose (LD50) of 364 μmol/kg via intraperitoneal administration.
Chemical Information
-
CAS No. 2072857-15-7
-
Molecular Weight 336.39
-
Formula C19H20N4O2
-
SMILES
OC1=CC=C(CCCCNC2=CC=NC3=CC=CC=C23)N=C1/C=N/O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)