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

L-745870 hydrochloride 

Cat. No.: HY-14325B Purity: 99.88%
Handling Instructions

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
10 mM * 1  mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 82 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

Molecular Weight

363.28

Formula

C₁₈H₂₀Cl₂N₄

CAS No.

1173023-36-3

SMILES

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

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 : 62.5 mg/mL (172.04 mM; Need ultrasonic)

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
10 mM 0.2753 mL 1.3763 mL 2.7527 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: ≥ 2.08 mg/mL (5.73 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.73 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

L-745870L745870L 745870Dopamine ReceptorHumandopamineD4receptorbrainpenetrationneurolepticsInhibitorinhibitorinhibit

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Product Name:
L-745870 hydrochloride
Cat. No.:
HY-14325B
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