L-745870 hydrochloride NEW
| Price | $34 | $59 | $113 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: L-745870 hydrochloride | CAS No.: 1173023-36-3 |
| Purity: 97.36% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | L-745870 hydrochloride |
| Description | L-745870 hydrochloride has excellent brain penetration.?L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM.? |
| In vitro | In vitro pharmacological studies revealed that L-745870 is an antagonist at human D4 receptors, in that L-745870 antagonized the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding,?blocked the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells,?blocked dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells,?inhibited D4 activation of cloned G protein-coupled inwardly rectifying K+ channels,?and antagonized dopamine-induced stimulation of extracellular acidification in transfected cells[1]. |
| In vivo | L-745870 exhibits favorable pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 of 2.1-2.8 hours) in both rats and monkeys, with excellent brain penetration and high brain-to-plasma ratios in rats[1]. Evaluation of L-745870 in surrogate marker assays indicates that it is readily available for biological activity in the brain and at doses of 5 to 60 mg/kg p.o., it would occupy 50% of D4 receptors in the brain. L-745870 does not affect apomorphine-induced stereotypy in rats but induces catalepsy in mice at a high dose of 100 mg/kg p.o., likely due to D2 receptor occupancy. Higher doses of L-745870 are anticipated to cause extrapyramidal symptoms in primates as these CNS levels would antagonize D2 receptors. In squirrel monkeys, L-745870 (10 mg/kg p.o.) induces mild sedation and at 30 mg/kg, it causes noticeable extrapyramidal motor symptoms, notably bradykinesia[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (151.4 mM), Sonication is recommended. 0.1 M HCL : 20 mg/mL (55.05 mM), when pH is adjusted to 3 with HCl. Sonication is recommended. |
| Keywords | L745870 | dopamine | L 745870 | inhibit | penetration | receptor | Human | L-745870 Hydrochloride | L 745870 Hydrochloride | brain | Inhibitor | neuroleptics | L-745870 | L745870 Hydrochloride | Dopamine Receptor | L 745870 hydrochloride | L745870 hydrochloride |
| Inhibitors Related | Olanzapine | CLOZAPINE N-OXIDE | Mirtazapine | Promazine hydrochloride | Octopamine hydrochloride | Octodrine | Citicoline | Phenothiazine | Oxolinic acid | Mianserin hydrochloride | Doxepin hydrochloride | Fluphenazine dihydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Parkinson's Disease Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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