2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. L-745870 hydrochloride

L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.

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

L-745870 hydrochloride Chemical Structure

L-745870 hydrochloride Chemical Structure

CAS No. : 1173023-36-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 120 In-stock
50 mg USD 380 In-stock
100 mg USD 550 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of L-745870 hydrochloride:

L-745870 hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].

IC50 & Target[3]

Human D4 Receptor

4.3 nM (Ki)

D2 Receptor

960 nM (Ki)

D3 Receptor

2300 mM (Ki)

In Vitro

L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells; inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1].

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

L-745870 hydrochloride Related Antibodies
In Vivo

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[1].
Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

363.28

Formula

C18H20Cl2N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.ClC(C=C1)=CC=C1N(CC2)CCN2CC3=CNC4=NC=CC=C43
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 32.26 mg/mL (88.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

0.1 M HCL : 25 mg/mL (68.82 mM; ultrasonic and adjust pH to 3 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7527 mL 13.7635 mL 27.5270 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.91%

COA (249 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
0.1 M HCL / DMSO 1 mM 2.7527 mL 13.7635 mL 27.5270 mL 68.8174 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 mL 13.7635 mL
10 mM 0.2753 mL 1.3763 mL 2.7527 mL 6.8817 mL
15 mM 0.1835 mL 0.9176 mL 1.8351 mL 4.5878 mL
20 mM 0.1376 mL 0.6882 mL 1.3763 mL 3.4409 mL
25 mM 0.1101 mL 0.5505 mL 1.1011 mL 2.7527 mL
30 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2939 mL
40 mM 0.0688 mL 0.3441 mL 0.6882 mL 1.7204 mL
50 mM 0.0551 mL 0.2753 mL 0.5505 mL 1.3763 mL
60 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1470 mL
DMSO 80 mM 0.0344 mL 0.1720 mL 0.3441 mL 0.8602 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

L-745870 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-7458701173023-36-3L745870L 745870Dopamine ReceptorHumandopamineD4receptorbrainpenetrationneurolepticsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
L-745870 hydrochloride
Cat. No.:
HY-14325B
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.