[CAS NO. 726174-00-1]  A-381393

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PRODUCTS SPECIFICATIONS [726174-00-1]

Distributor
Catalog
AS893386
Brand
Arctom Scientific
CAS
726174-00-1

DESCRIPTION [726174-00-1]

Overview

MDL-
Molecular Weight320.43
Molecular FormulaC20H24N4
SMILESCC1=CC=C(C=C1C)N2CCN(CC2)CC3=NC4=CC=CC=C4N3

For research use only. We do not sell to patients.

Summary

A-381393 is a potent, selective, brain penetrate dopamine D 4 receptor antagonist, with K i s of 1.5, 1.9 and 1.6 nM for human dopamine D 4.4 , D 4.2 , and D 4.7 receptor, respectively, >2700-fold selectivity over D 1 , D 2 , D 3 and D 5 dopamine receptors. A-381393 shows moderate affinity for 5-HT 2A (K i , 370 nM) [1] .


IC50 & Target

Ki: 1.5 nM (D 4.4 receptor), 1.9 nM (D 4.2 receptor), 1.6 nM (D 4.7 receptor) [1]


In Vitro

A-381393 exhibits weak affinity at 5-HT 1A , Sigma 2, Adenoceptor α 1A , Adenoceptor α 2C , Histamine H1, with K i s of 1365, 8600, 2044, 1912 and 2962 nM, respectively [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 51.67 mg/mL ( 161.25 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1208 mL 15.6040 mL 31.2081 mL
5 mM 0.6242 mL 3.1208 mL 6.2416 mL
10 mM 0.3121 mL 1.5604 mL 3.1208 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

* All of the co-solvents are available by MCE.